Anticancer carbonic anhydrase inhibitors: A patent review (2008-2013) (468 views)
Expert Opin Ther Pat (ISSN: 1354-3776, 1744-7674electronic), 2013 Jun; 23(6): 737-749.
Export to BibTeX Export to EndNote
Paper type: Journal Article,
Impact factor: 3.441, 5-year impact factor: 2.921
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-84878067755&partnerID=40&md5=32a6f65c51a11a9a5f88621c8c64690f
Keywords: Anticancer Drugs, Ca Ix, Ca Xii, Carbonic Anhydrase, Coumarin, Hypoxia, Sulfamate, Sulfamide, Sulfonamide, Thiocoumarin, Carbonate Dehydratase Inhibitor, Carbonate Dehydratase Ix Inhibitor, Unclassified Drug, Antineoplastic Activity, Cancer Inhibition, Drug Potency, Drug Selectivity, Enzyme Inhibition, Human, Review, Structure Activity Relation, Animals, Antigens, Antineoplastic Agents, Carbonic Anhydrase Inhibitors, Disease Progression, Drug Design, Patents As Topic,
Affiliations:
*** IBB - CNR ***
Istituto di Biostrutture e Bioimmagini-CNR, via Mezzocannone 16, 80134 Naples, Italy
Università Degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy
References:
Alterio, V., Di Fiore, A., D'Ambrosio, K., Multiple binding modes of inhibitors to carbonic anhydrases: How to design specific drugs targeting 15 different isoforms? (2012) Chem Rev, 112, pp. 4421-446
Supuran, C., Carbonic anhydrases: Catalytic and inhibition mechanisms distribution and physiological roles (2004) Carbonic Anhydrase: Its Inhibitors and Activators, pp. 1-23. , Supuran CT Scozzafava A Conway J editors CRC Press, Boca Raton, FL
Supuran, C.T., Carbonic anhydrases: Novel therapeutic applications for inhibitors and activators (2008) Nat Rev Drug Discov, 7, pp. 168-181
Guler, O.O., De Simone, G., Supuran, C.T., Drug design studies of the novel antitumor targets carbonic anhydrase IX and XII (2010) Curr Med Chem, 17, pp. 1516-1526
Pastoreková, S., Pastorek, J., Cancer-related carbonic anhydrase isoenzymes and their inhibition (2004) Carbonic Anhydrase: Its Inhibitors and Activators, pp. 255-281. , Supuran CT Scozzafava A Conway J editors CRC Press, Boca Raton, FL
Ivanov, S., Liao, S.Y., Ivanova, A., Expression of hypoxia-inducible cellsurface transmembrane carbonic anhydrases in human cancer (2001) Am J Pathol, 158, pp. 905-919
Pastorekova, S., Zatovicova, M., Pastorek, J., Cancer-associated carbonic anhydrases and their inhibition (2008) Curr Pharm des, 14, pp. 685-698
Supuran, C.T., Di Fiore, A., Alterio, V., Recent advances in structural studies of the carbonic anhydrase family: The crystal structure of human CA IX and CA XIII (2010) Curr Pharm des, 16, pp. 3246-3254
Stillebroer, A.B., Mulders, P.F., Boerman, O.C., Carbonic anhydrase IX in renal cell carcinoma: Implications for prognosis, diagnosis, and therapy (2010) Eur Urol, 58, pp. 75-83
Monti, S.M., Supuran, C.T., De Simone, G., Carbonic anhydrase IX as a target for designing novel anticancer drugs (2012) Curr Med Chem, 19, pp. 821-830
Opavský, R., Pastoreková, S., Zelńk, V., Human MN/CA9 gene, a novel member of the carbonic anhydrase family: Structure and exon to protein domain relationships (1996) Genomics, 33, pp. 480-487
Pastorek, J., Pastoreková, S., Callebaut, I., Cloning and characterization of MN, a human tumor-associated protein with a domain homologous to carbonic anhydrase and a putative helix-loop-helix DNA binding segment (1994) Oncogene, 9, pp. 2877-2888
Wykoff, C.C., Beasley, N.J., Watson, P.H., Hypoxia-inducible expression of tumor-associated carbonic anhydrases (2000) Cancer Res, 60, pp. 7075-7083
Potter, C., Harris, A.L., Hypoxia inducible carbonic anhydrase IX, marker of tumour hypoxia, survival pathway and therapy target (2004) Cell Cycle, 3, pp. 164-167
Pastorekova, S., Barathova, M., Kopacek, J., Pastorek, J., Carbonic anhydrase inhibitors targeting cancer: Therapeutic immunologic and diagnostic tools targeting isoforms IX and XII (2009) Drug Design of Zinc-enzyme Inhibitors: Functional Structural and Disease Applications, pp. 193-222. , Supuran CT Winum JY editors Hoboken Wiley New Jersey
Swietach, P., Vaughan-Jones, R.D., Harris, A.L., Regulation of tumor pH and the role of carbonic anhydrase (2007) Cancer Metastasis Rev, 26, pp. 299-310
Stubbs, M., McSheehy, P.M., Griffiths, J.R., Bashford, C.L., Causes and consequences of tumor acidity and implications for treatment (2000) Mol Med Today, 6, pp. 15-19
Helmlinger, G., Sckell, A., Dellian, M., Acid production in glycolysis-impaired tumors provides new insights into tumor metabolism (2002) Clin Cancer Res, 8, pp. 1284-1291
Fukumura, D., Jain, R.K., Tumor microenvironment abnormalities: Causes, consequences, and strategies to normalize (2007) J Cell Biochem, 101, pp. 937-949
Lee, A.H., Tannock, I.F., Heterogeneity of intracellular pH and of mechanisms that regulate intracellular pH in populations of cultured cells (1998) Cancer Res, 58, pp. 1901-1908
Chiche, J., Brahimi-Horn, M.C., Pouysségur, J., Tumour hypoxia induces a metabolic shift causing acidosis: A common feature in cancer (2010) J Cell Mol Med, 14, pp. 771-794
Svastova, E., Zilka, N., Zat'Ovicova, M., Carbonic anhydrase IX reduces E-cadherin-mediated adhesion of MDCK cells via interaction with beta-catenin (2003) Exp Cell Res, 290, pp. 332-345
Zavadova, Z., Zavada, J., Carbonic anhydrase IX (CA IX) mediates tumor cell interactions with microenvironment (2005) Oncol Rep, 13, pp. 977-982
Zavada, J., Zavadova, Z., Pastorek, J., Human tumour-associated cell adhesion protein MN/CA IX: Identification of M75 epitope and of the region mediating cell adhesion (2000) Br J Cancer, 82, pp. 1808-1813
Innocenti, A., Pastorekova, S., Pastorek, J., The proteoglycan region of the tumor-associated carbonic anhydrase isoform IX acts as an intrinsic buffer optimizing CO2 hydration at acidic pH values characteristic of solid tumors (2009) Bioorg Med Chem Lett, 19, pp. 5825-5828
Alterio, V., Hilvo, M., Di Fiore, A., Crystal structure of the catalytic domain of the tumor-associated human carbonic anhydrase IX (2009) Proc Natl Acad Sci USA, 106, pp. 16233-16238
Ditte, P., Dequiedt, F., Svastova, E., Phosphorylation of carbonic anhydrase IX controls its ability to mediate extracellular acidification in hypoxic tumors (2011) Cancer Res, 71, pp. 7558-7567
Dorai, T., Sawczuk, I.S., Pastorek, J., The role of carbonic anhydrase IX overexpression in kidney cancer (2005) Eur J Cancer, 41, pp. 2935-2947
Hulikova, A., Zatovicova, M., Svastova, E., Intact intracellular tail is critical for proper functioning of the tumor-associated, hypoxia-regulated carbonic anhydrase IX (2009) FEBS Lett, 583, pp. 3563-3568
Buanne, P., Renzone, G., Monteleone, F., Characterization of carbonic anhydrase IX interactome reveals proteins assisting its nuclear localization in hypoxic cells (2013) J Proteome Res, 12, pp. 282-292
Hilvo, M., Baranauskiene, L., Salzano, A.M., Biochemical characterization of CA IX, one of the most active carbonic anhydrase isozymes (2008) J Biol Chem, 283, pp. 27799-27809
Türeci, O., Sahin, U., Vollmar, E., Human carbonic anhydrase XII: CDNA cloning, expression, and chromosomal localization of a carbonic anhydrase gene that is overexpressed in some renal cell cancers (1998) Proc Natl Acad Sci USA, 95, pp. 7608-7613
Ivanov, S.V., Kuzmin, I., Wei, M.H., Down-regulation of transmembrane carbonic anhydrases in renal cell carcinoma cell lines by wild-type von Hippel-Lindau transgenes (1998) Proc Natl Acad Sci USA, 95, pp. 12596-12601
Hynninen, P., Vaskivuo, L., Saarnio, J., Expression of transmembrane carbonic anhydrases IX and XII in ovarian tumours (2006) Histopathology, 49, pp. 594-602
Kim, J.Y., Shin, H.J., Kim, T.H., Tumor-associated carbonic anhydrases are linked to metastases in primary cervical cancer (2006) J Cancer Res Clin Oncol, 132, pp. 302-308
Chiche, J., Ilc, K., Laferrière, J., Hypoxia-inducible carbonic anhydrase IX and XII promote tumor cell growth by counteracting acidosis through the regulation of the intracellular pH (2009) Cancer Res, 69, pp. 358-368
Haapasalo, J., Hilvo, M., Nordfors, K., Identification of an alternatively spliced isoform of carbonic anhydrase XII in diffusely infiltrating astrocytic gliomas (2008) Neuro Oncol, 10, pp. 131-138
Hsieh, M.J., Chen, K.S., Chiou, H.L., Hsieh, Y.S., Carbonic anhydrase XII promotes invasion and migration ability of MDA-MB-231 breast cancer cells through the p38 MAPK signaling pathway (2010) Eur J Cell Biol, 89, pp. 598-606
Kivela, A.J., Parkkila, S., Saarnio, J., Expression of transmembrane carbonic anhydrase isoenzymes IX and XII in normal human pancreas and pancreatic tumours (2000) Histochem Cell Biol, 114, pp. 197-204
Kivela, A., Parkkila, S., Saarnio, J., Expression of a novel transmembrane carbonic anhydrase isozyme XII in normal human gut and colorectal tumors (2000) Am J Pathol, 156, pp. 577-584
Ilie, M.I., Hofman, V., Ortholan, C., Overexpression of carbonic anhydrase XII in tissues from resectable non-small cell lung cancers is a biomarker of good prognosis (2011) Int J Cancer, 128, pp. 1614-1623
Karhumaa, P., Parkkila, S., Türeci, O., Identification of carbonic anhydrase XII as the membrane isozyme expressed in the normal human endometrial epithelium (2000) Mol Hum Reprod, 6, pp. 68-74
Parkkila, S., Parkkila, A.K., Saarnio, J., Expression of the membrane-associated carbonic anhydrase isozyme XII in the human kidney and renal tumors (2000) J Histochem Cytochem, 48, pp. 1601-1608
Liao, S.Y., Ivanov, S., Ivanova, A., Expression of cell surface transmembrane carbonic anhydrase genes CA9 and CA12 in the human eye: Overexpression of CA12 (CAXII) in glaucoma (2003) J Med Genet, 40, pp. 257-261
Hussain, S.A., Ganesan, R., Reynolds, G., Hypoxia-regulated carbonic anhydrase IX expression is associated with poor survival in patients with invasive breast cancer (2007) Br J Cancer, 96, pp. 104-109
Whittington, D.A., Waheed, A., Ulmasov, B., Crystal structure of the dimeric extracellular domain of human carbonic anhydrase XII, a bitopic membrane protein overexpressed in certain cancer tumor cells (2001) Proc Natl Acad Sci USA, 98, pp. 9545-9550
Svastová, E., Huĺková, A., Rafajová, M., Hypoxia activates the capacity of tumor-associated carbonic anhydrase IX to acidify extracellular pH (2004) FEBS Lett, 577, pp. 439-445
Cecchi, A., Hulikova, A., Pastorek, J., Carbonic anhydrase inhibitors. Design of fluorescent sulfonamides as probes of tumor-associated carbonic anhydrase IX that inhibit isozyme IX-mediated acidification of hypoxic tumors (2005) J Med Chem, 48, pp. 4834-4841
Scozzafava, A., Mastrolorenzo, A., Supuran, C.T., Modulation of carbonic anhydrase activity and its applications in therapy (2004) Expert Opin Ther Pat, 14, pp. 667-702
Supuran, C.T., Scozzafava, A., Casini, A., Carbonic anhydrase inhibitors (2003) Med Res Rev, 23, pp. 146-189
Pastorekova, S., Casini, A., Scozzafava, A., Carbonic anhydrase inhibitors: The first selective, membrane-impermeant inhibitors targeting the tumor-associated isozyme IX (2004) Bioorg Med Chem Lett, 14, pp. 869-873
Thiry, A., Dogné, J.-M., Masereel, B., Supuran, C.T., Targeting tumor-associated carbonic anhydrase IX in cancer therapy (2006) Trends Pharmacol Sci, 27, pp. 566-573
Carta, F., Scozzafava, A., Supuran, C.T., Sulfonamides: A patent review 2008-2012 (2012) Expert Opin Ther Pat, 22, pp. 747-758
Nicox, S.A., Supuran, C.T., Benedini, F., (2008) Nitrate Esters of Carbonic Anhydrase Inhibitors, , WO071421
Dubois, L.J., Lambin, P., (2012) Cancer Targeting Using Carbonic Anhydrase Isoform IX Inhibitors, , Stichting Maastricht Radiation Oncology Maastro Clinic WO087115
Zimmerman, C., Babich, J.W., (2009) Inhibitors of Carbonic Anhydrase IX, , Molecular Insight Pharm Inc WO089383
(2011) Carbonic Anhydrase Inhibitors, , Univ Firenze, Uni Oslo, Univ Manchester et al. WO098610
Masereel, B., Frederick, R., Supuran, C.T., (2012) Tetraline Sulfonamide Derivatives for Use in the Treatment of Proliferative Disorders, , Univ Notre Dame de la Paix WO175654
(2010) Sulfonamide Inhibitors of Carbonic Anhydrase, , Auspex Pharmaceuticals Inc US2010317655
Casey, J.R., Morgan, P.E., Vullo, D., Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX (2004) J Med Chem, 47, pp. 2337-2347
Scozzafava, A., Briganti, F., Ilies, M.A., Supuran, C.T., Carbonic anhydrase inhibitors: Synthesis of membrane-impermeant low molecular weight sulfonamides possessing in vivo selectivity for the membrane-bound versus cytosolic isozymes (2000) J Med Chem, 43, pp. 292-300
(2008) CA IX-specific Inhibitors, , Institute of Virology of the Slovak Academy of Sciences US095707
Scozzafava, A., (2012) CA IX-specific Inhibitors, , Institute of Virology Supuran CT AU211499
Supuran, C., Scozzafava, A., (2010) CA IX-specific Inhibitors, , Institute of Virology AU200368
Dubois, L., Douma, K., Supuran, C.T., Imaging the hypoxia surrogate marker CA IX requires expression and catalytic activity for binding fluorescent sulfonamide inhibitors (2007) Radiother Oncol, 83, pp. 367-373
Dubois, L., Lieuwes, N.G., Maresca, A., Imaging of CA IX with fluorescent labelled sulfonamides distinguishes hypoxic and (re)-oxygenated cells in a xenograft tumour model (2009) Radiother Oncol, 92, pp. 423-428
(2008) Sulfonamide Derivatives Having Carbonic Anhydrase Inhibiting Activity and Their Use As Therapeutic and Diagnostic Agents, , Union Life Sciences Ltd US138291
Pacchiano, F., Aggarwal, M., Avvaru, B.S., Selective hydrophobic pocket binding observed within the carbonic anhydrase II active site accommodate different 4-substituted- ureidobenzenesulfonamides and correlate to inhibitor potency (2010) Chem Commun (Camb, 46, pp. 8371-8373
Pacchiano, F., Carta, F., McDonald, P.C., Ureido-substituted benzenesulfonamides potently inhibit carbonic anhydrase IX and show antimetastatic activity in a model of breast cancer metastasis (2011) J Med Chem, 54, pp. 1896-1902
Supuran, C., Dedhar, S., (2012) Novel Sulfonamide Compounds for Inhibition of Metastatic Tumor Growth, , MetaSignal Therapeutics Inc WO021963
Maresca, A., Temperini, C., Vu, H., Non-zinc mediated inhibition of carbonic anhydrases: Coumarins are a new class of suicide inhibitors (2009) J Am Chem Soc, 131, pp. 3057-3062
Maresca, A., Scozzafava, A., Supuran, C.T., 7,8-disubstituted-but not 6,7-disubstituted coumarins selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic ones i and II in the low nanomolar/subnanomolar range (2010) Bioorg Med Chem Lett, 20, pp. 7255-7258
Lou, Y., McDonald, P.C., Oloumi, A., Targeting tumor hypoxia: Suppression of breast tumor growth and metastasis by novel carbonic anhydrase IX inhibitors (2011) Cancer Res, 71, pp. 3364-3376
Lock, F.E., McDonald, P.C., Lou, Y., Targeting carbonic anhydrase IX depletes breast cancer stem cells within the hypoxic niche (2012) Oncogene, , doi: 10.1038/onc.2012.550
Vu, H., Pham, N.B., Quinn, R.J., Direct screening of natural product extracts using mass spectrometry (2008) J Biomol Screen, 13, pp. 265-275
Maresca, A., Supuran, C.T., Coumarins incorporating hydroxy-and chloro-moieties selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic ones i and II (2010) Bioorg Med Chem Lett, 20, pp. 4511-4514
Supuran, C.T., Parkkila, S., (2010) Treatment of Mammalian Disorders Mediated by Alpha-carbonic Anhydrase Isoforms, , Univ Tampere WO139678
Parkkila, S., Innocenti, A., Kallio, H., The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms (2009) Bioorg Med Chem Lett, 19, pp. 4102-4106
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Expert Opin Ther Pat (ISSN: 1354-3776, 1744-7674electronic), 2013 Jun; 23(6): 737-749.
Export to BibTeX Export to EndNote
Paper type: Journal Article,
Impact factor: 3.441, 5-year impact factor: 2.921
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-84878067755&partnerID=40&md5=32a6f65c51a11a9a5f88621c8c64690f
Keywords: Anticancer Drugs, Ca Ix, Ca Xii, Carbonic Anhydrase, Coumarin, Hypoxia, Sulfamate, Sulfamide, Sulfonamide, Thiocoumarin, Carbonate Dehydratase Inhibitor, Carbonate Dehydratase Ix Inhibitor, Unclassified Drug, Antineoplastic Activity, Cancer Inhibition, Drug Potency, Drug Selectivity, Enzyme Inhibition, Human, Review, Structure Activity Relation, Animals, Antigens, Antineoplastic Agents, Carbonic Anhydrase Inhibitors, Disease Progression, Drug Design, Patents As Topic,
Affiliations:
*** IBB - CNR ***
Istituto di Biostrutture e Bioimmagini-CNR, via Mezzocannone 16, 80134 Naples, Italy
Università Degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy
References:
Alterio, V., Di Fiore, A., D'Ambrosio, K., Multiple binding modes of inhibitors to carbonic anhydrases: How to design specific drugs targeting 15 different isoforms? (2012) Chem Rev, 112, pp. 4421-446
Supuran, C., Carbonic anhydrases: Catalytic and inhibition mechanisms distribution and physiological roles (2004) Carbonic Anhydrase: Its Inhibitors and Activators, pp. 1-23. , Supuran CT Scozzafava A Conway J editors CRC Press, Boca Raton, FL
Supuran, C.T., Carbonic anhydrases: Novel therapeutic applications for inhibitors and activators (2008) Nat Rev Drug Discov, 7, pp. 168-181
Guler, O.O., De Simone, G., Supuran, C.T., Drug design studies of the novel antitumor targets carbonic anhydrase IX and XII (2010) Curr Med Chem, 17, pp. 1516-1526
Pastoreková, S., Pastorek, J., Cancer-related carbonic anhydrase isoenzymes and their inhibition (2004) Carbonic Anhydrase: Its Inhibitors and Activators, pp. 255-281. , Supuran CT Scozzafava A Conway J editors CRC Press, Boca Raton, FL
Ivanov, S., Liao, S.Y., Ivanova, A., Expression of hypoxia-inducible cellsurface transmembrane carbonic anhydrases in human cancer (2001) Am J Pathol, 158, pp. 905-919
Pastorekova, S., Zatovicova, M., Pastorek, J., Cancer-associated carbonic anhydrases and their inhibition (2008) Curr Pharm des, 14, pp. 685-698
Supuran, C.T., Di Fiore, A., Alterio, V., Recent advances in structural studies of the carbonic anhydrase family: The crystal structure of human CA IX and CA XIII (2010) Curr Pharm des, 16, pp. 3246-3254
Stillebroer, A.B., Mulders, P.F., Boerman, O.C., Carbonic anhydrase IX in renal cell carcinoma: Implications for prognosis, diagnosis, and therapy (2010) Eur Urol, 58, pp. 75-83
Monti, S.M., Supuran, C.T., De Simone, G., Carbonic anhydrase IX as a target for designing novel anticancer drugs (2012) Curr Med Chem, 19, pp. 821-830
Opavský, R., Pastoreková, S., Zelńk, V., Human MN/CA9 gene, a novel member of the carbonic anhydrase family: Structure and exon to protein domain relationships (1996) Genomics, 33, pp. 480-487
Pastorek, J., Pastoreková, S., Callebaut, I., Cloning and characterization of MN, a human tumor-associated protein with a domain homologous to carbonic anhydrase and a putative helix-loop-helix DNA binding segment (1994) Oncogene, 9, pp. 2877-2888
Wykoff, C.C., Beasley, N.J., Watson, P.H., Hypoxia-inducible expression of tumor-associated carbonic anhydrases (2000) Cancer Res, 60, pp. 7075-7083
Potter, C., Harris, A.L., Hypoxia inducible carbonic anhydrase IX, marker of tumour hypoxia, survival pathway and therapy target (2004) Cell Cycle, 3, pp. 164-167
Pastorekova, S., Barathova, M., Kopacek, J., Pastorek, J., Carbonic anhydrase inhibitors targeting cancer: Therapeutic immunologic and diagnostic tools targeting isoforms IX and XII (2009) Drug Design of Zinc-enzyme Inhibitors: Functional Structural and Disease Applications, pp. 193-222. , Supuran CT Winum JY editors Hoboken Wiley New Jersey
Swietach, P., Vaughan-Jones, R.D., Harris, A.L., Regulation of tumor pH and the role of carbonic anhydrase (2007) Cancer Metastasis Rev, 26, pp. 299-310
Stubbs, M., McSheehy, P.M., Griffiths, J.R., Bashford, C.L., Causes and consequences of tumor acidity and implications for treatment (2000) Mol Med Today, 6, pp. 15-19
Helmlinger, G., Sckell, A., Dellian, M., Acid production in glycolysis-impaired tumors provides new insights into tumor metabolism (2002) Clin Cancer Res, 8, pp. 1284-1291
Fukumura, D., Jain, R.K., Tumor microenvironment abnormalities: Causes, consequences, and strategies to normalize (2007) J Cell Biochem, 101, pp. 937-949
Lee, A.H., Tannock, I.F., Heterogeneity of intracellular pH and of mechanisms that regulate intracellular pH in populations of cultured cells (1998) Cancer Res, 58, pp. 1901-1908
Chiche, J., Brahimi-Horn, M.C., Pouysségur, J., Tumour hypoxia induces a metabolic shift causing acidosis: A common feature in cancer (2010) J Cell Mol Med, 14, pp. 771-794
Svastova, E., Zilka, N., Zat'Ovicova, M., Carbonic anhydrase IX reduces E-cadherin-mediated adhesion of MDCK cells via interaction with beta-catenin (2003) Exp Cell Res, 290, pp. 332-345
Zavadova, Z., Zavada, J., Carbonic anhydrase IX (CA IX) mediates tumor cell interactions with microenvironment (2005) Oncol Rep, 13, pp. 977-982
Zavada, J., Zavadova, Z., Pastorek, J., Human tumour-associated cell adhesion protein MN/CA IX: Identification of M75 epitope and of the region mediating cell adhesion (2000) Br J Cancer, 82, pp. 1808-1813
Innocenti, A., Pastorekova, S., Pastorek, J., The proteoglycan region of the tumor-associated carbonic anhydrase isoform IX acts as an intrinsic buffer optimizing CO2 hydration at acidic pH values characteristic of solid tumors (2009) Bioorg Med Chem Lett, 19, pp. 5825-5828
Alterio, V., Hilvo, M., Di Fiore, A., Crystal structure of the catalytic domain of the tumor-associated human carbonic anhydrase IX (2009) Proc Natl Acad Sci USA, 106, pp. 16233-16238
Ditte, P., Dequiedt, F., Svastova, E., Phosphorylation of carbonic anhydrase IX controls its ability to mediate extracellular acidification in hypoxic tumors (2011) Cancer Res, 71, pp. 7558-7567
Dorai, T., Sawczuk, I.S., Pastorek, J., The role of carbonic anhydrase IX overexpression in kidney cancer (2005) Eur J Cancer, 41, pp. 2935-2947
Hulikova, A., Zatovicova, M., Svastova, E., Intact intracellular tail is critical for proper functioning of the tumor-associated, hypoxia-regulated carbonic anhydrase IX (2009) FEBS Lett, 583, pp. 3563-3568
Buanne, P., Renzone, G., Monteleone, F., Characterization of carbonic anhydrase IX interactome reveals proteins assisting its nuclear localization in hypoxic cells (2013) J Proteome Res, 12, pp. 282-292
Hilvo, M., Baranauskiene, L., Salzano, A.M., Biochemical characterization of CA IX, one of the most active carbonic anhydrase isozymes (2008) J Biol Chem, 283, pp. 27799-27809
Türeci, O., Sahin, U., Vollmar, E., Human carbonic anhydrase XII: CDNA cloning, expression, and chromosomal localization of a carbonic anhydrase gene that is overexpressed in some renal cell cancers (1998) Proc Natl Acad Sci USA, 95, pp. 7608-7613
Ivanov, S.V., Kuzmin, I., Wei, M.H., Down-regulation of transmembrane carbonic anhydrases in renal cell carcinoma cell lines by wild-type von Hippel-Lindau transgenes (1998) Proc Natl Acad Sci USA, 95, pp. 12596-12601
Hynninen, P., Vaskivuo, L., Saarnio, J., Expression of transmembrane carbonic anhydrases IX and XII in ovarian tumours (2006) Histopathology, 49, pp. 594-602
Kim, J.Y., Shin, H.J., Kim, T.H., Tumor-associated carbonic anhydrases are linked to metastases in primary cervical cancer (2006) J Cancer Res Clin Oncol, 132, pp. 302-308
Chiche, J., Ilc, K., Laferrière, J., Hypoxia-inducible carbonic anhydrase IX and XII promote tumor cell growth by counteracting acidosis through the regulation of the intracellular pH (2009) Cancer Res, 69, pp. 358-368
Haapasalo, J., Hilvo, M., Nordfors, K., Identification of an alternatively spliced isoform of carbonic anhydrase XII in diffusely infiltrating astrocytic gliomas (2008) Neuro Oncol, 10, pp. 131-138
Hsieh, M.J., Chen, K.S., Chiou, H.L., Hsieh, Y.S., Carbonic anhydrase XII promotes invasion and migration ability of MDA-MB-231 breast cancer cells through the p38 MAPK signaling pathway (2010) Eur J Cell Biol, 89, pp. 598-606
Kivela, A.J., Parkkila, S., Saarnio, J., Expression of transmembrane carbonic anhydrase isoenzymes IX and XII in normal human pancreas and pancreatic tumours (2000) Histochem Cell Biol, 114, pp. 197-204
Kivela, A., Parkkila, S., Saarnio, J., Expression of a novel transmembrane carbonic anhydrase isozyme XII in normal human gut and colorectal tumors (2000) Am J Pathol, 156, pp. 577-584
Ilie, M.I., Hofman, V., Ortholan, C., Overexpression of carbonic anhydrase XII in tissues from resectable non-small cell lung cancers is a biomarker of good prognosis (2011) Int J Cancer, 128, pp. 1614-1623
Karhumaa, P., Parkkila, S., Türeci, O., Identification of carbonic anhydrase XII as the membrane isozyme expressed in the normal human endometrial epithelium (2000) Mol Hum Reprod, 6, pp. 68-74
Parkkila, S., Parkkila, A.K., Saarnio, J., Expression of the membrane-associated carbonic anhydrase isozyme XII in the human kidney and renal tumors (2000) J Histochem Cytochem, 48, pp. 1601-1608
Liao, S.Y., Ivanov, S., Ivanova, A., Expression of cell surface transmembrane carbonic anhydrase genes CA9 and CA12 in the human eye: Overexpression of CA12 (CAXII) in glaucoma (2003) J Med Genet, 40, pp. 257-261
Hussain, S.A., Ganesan, R., Reynolds, G., Hypoxia-regulated carbonic anhydrase IX expression is associated with poor survival in patients with invasive breast cancer (2007) Br J Cancer, 96, pp. 104-109
Whittington, D.A., Waheed, A., Ulmasov, B., Crystal structure of the dimeric extracellular domain of human carbonic anhydrase XII, a bitopic membrane protein overexpressed in certain cancer tumor cells (2001) Proc Natl Acad Sci USA, 98, pp. 9545-9550
Svastová, E., Huĺková, A., Rafajová, M., Hypoxia activates the capacity of tumor-associated carbonic anhydrase IX to acidify extracellular pH (2004) FEBS Lett, 577, pp. 439-445
Cecchi, A., Hulikova, A., Pastorek, J., Carbonic anhydrase inhibitors. Design of fluorescent sulfonamides as probes of tumor-associated carbonic anhydrase IX that inhibit isozyme IX-mediated acidification of hypoxic tumors (2005) J Med Chem, 48, pp. 4834-4841
Scozzafava, A., Mastrolorenzo, A., Supuran, C.T., Modulation of carbonic anhydrase activity and its applications in therapy (2004) Expert Opin Ther Pat, 14, pp. 667-702
Supuran, C.T., Scozzafava, A., Casini, A., Carbonic anhydrase inhibitors (2003) Med Res Rev, 23, pp. 146-189
Pastorekova, S., Casini, A., Scozzafava, A., Carbonic anhydrase inhibitors: The first selective, membrane-impermeant inhibitors targeting the tumor-associated isozyme IX (2004) Bioorg Med Chem Lett, 14, pp. 869-873
Thiry, A., Dogné, J.-M., Masereel, B., Supuran, C.T., Targeting tumor-associated carbonic anhydrase IX in cancer therapy (2006) Trends Pharmacol Sci, 27, pp. 566-573
Carta, F., Scozzafava, A., Supuran, C.T., Sulfonamides: A patent review 2008-2012 (2012) Expert Opin Ther Pat, 22, pp. 747-758
Nicox, S.A., Supuran, C.T., Benedini, F., (2008) Nitrate Esters of Carbonic Anhydrase Inhibitors, , WO071421
Dubois, L.J., Lambin, P., (2012) Cancer Targeting Using Carbonic Anhydrase Isoform IX Inhibitors, , Stichting Maastricht Radiation Oncology Maastro Clinic WO087115
Zimmerman, C., Babich, J.W., (2009) Inhibitors of Carbonic Anhydrase IX, , Molecular Insight Pharm Inc WO089383
(2011) Carbonic Anhydrase Inhibitors, , Univ Firenze, Uni Oslo, Univ Manchester et al. WO098610
Masereel, B., Frederick, R., Supuran, C.T., (2012) Tetraline Sulfonamide Derivatives for Use in the Treatment of Proliferative Disorders, , Univ Notre Dame de la Paix WO175654
(2010) Sulfonamide Inhibitors of Carbonic Anhydrase, , Auspex Pharmaceuticals Inc US2010317655
Casey, J.R., Morgan, P.E., Vullo, D., Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX (2004) J Med Chem, 47, pp. 2337-2347
Scozzafava, A., Briganti, F., Ilies, M.A., Supuran, C.T., Carbonic anhydrase inhibitors: Synthesis of membrane-impermeant low molecular weight sulfonamides possessing in vivo selectivity for the membrane-bound versus cytosolic isozymes (2000) J Med Chem, 43, pp. 292-300
(2008) CA IX-specific Inhibitors, , Institute of Virology of the Slovak Academy of Sciences US095707
Scozzafava, A., (2012) CA IX-specific Inhibitors, , Institute of Virology Supuran CT AU211499
Supuran, C., Scozzafava, A., (2010) CA IX-specific Inhibitors, , Institute of Virology AU200368
Dubois, L., Douma, K., Supuran, C.T., Imaging the hypoxia surrogate marker CA IX requires expression and catalytic activity for binding fluorescent sulfonamide inhibitors (2007) Radiother Oncol, 83, pp. 367-373
Dubois, L., Lieuwes, N.G., Maresca, A., Imaging of CA IX with fluorescent labelled sulfonamides distinguishes hypoxic and (re)-oxygenated cells in a xenograft tumour model (2009) Radiother Oncol, 92, pp. 423-428
(2008) Sulfonamide Derivatives Having Carbonic Anhydrase Inhibiting Activity and Their Use As Therapeutic and Diagnostic Agents, , Union Life Sciences Ltd US138291
Pacchiano, F., Aggarwal, M., Avvaru, B.S., Selective hydrophobic pocket binding observed within the carbonic anhydrase II active site accommodate different 4-substituted- ureidobenzenesulfonamides and correlate to inhibitor potency (2010) Chem Commun (Camb, 46, pp. 8371-8373
Pacchiano, F., Carta, F., McDonald, P.C., Ureido-substituted benzenesulfonamides potently inhibit carbonic anhydrase IX and show antimetastatic activity in a model of breast cancer metastasis (2011) J Med Chem, 54, pp. 1896-1902
Supuran, C., Dedhar, S., (2012) Novel Sulfonamide Compounds for Inhibition of Metastatic Tumor Growth, , MetaSignal Therapeutics Inc WO021963
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Maresca, A., Scozzafava, A., Supuran, C.T., 7,8-disubstituted-but not 6,7-disubstituted coumarins selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic ones i and II in the low nanomolar/subnanomolar range (2010) Bioorg Med Chem Lett, 20, pp. 7255-7258
Lou, Y., McDonald, P.C., Oloumi, A., Targeting tumor hypoxia: Suppression of breast tumor growth and metastasis by novel carbonic anhydrase IX inhibitors (2011) Cancer Res, 71, pp. 3364-3376
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Supuran, C.T., Parkkila, S., (2010) Treatment of Mammalian Disorders Mediated by Alpha-carbonic Anhydrase Isoforms, , Univ Tampere WO139678
Parkkila, S., Innocenti, A., Kallio, H., The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms (2009) Bioorg Med Chem Lett, 19, pp. 4102-4106
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Anticancer carbonic anhydrase inhibitors: A patent review (2008-2013)
Introduction: Human carbonic anhydrases (EC 4.2.1.1) IX (hCA IX) and XII (hCA XII) are two tumor-associated proteins, being overexpressed in many tumors and involved in critical processes associated with cancer progression and response to therapy. Both are multi-domain proteins consisting of an extracellular catalytic domain (CA), a transmembrane portion (TM) and an intracytoplasmic (IC) segment. These domains have peculiar biochemical and physiological features. CA IX contains an additional proteoglycan-like (PG) domain at the N-terminus which constitutes a unique feature of this enzyme within the CA family. Areas covered: Starting from a brief description of the main molecular and catalytic features of both enzymes, their role in tumor physiology and their three-dimensional structure, this review describes the main classes of small molecule inhibitors, investigated between 2008 and 2013, able to inhibit these enzymes for both diagnostic and therapeutic applications. Expert opinion: A consistent number of patents on molecules able to inhibit the catalytic activity of CA IX and CA XII have been recently reported. Most patents deal with classical sulfonamide derivatives, demonstrating that introducing suitable substituents on the inhibitor scaffold, good selectivity can be obtained. However, the most impressive results are related to compounds containing novel chemotypes, such as coumarins and thiocumarins. Thus, it is expected that research in next future will be more dedicated to the development of molecules containing new chemotypes and a large number of studies in such field have already been published demonstrating the role of these enzymes in carcinogenesis and metastases formation. © 2013 Informa UK, Ltd.
Introduction: Human carbonic anhydrases (EC 4.2.1.1) IX (hCA IX) and XII (hCA XII) are two tumor-associated proteins, being overexpressed in many tumors and involved in critical processes associated with cancer progression and response to therapy. Both are multi-domain proteins consisting of an extracellular catalytic domain (CA), a transmembrane portion (TM) and an intracytoplasmic (IC) segment. These domains have peculiar biochemical and physiological features. CA IX contains an additional proteoglycan-like (PG) domain at the N-terminus which constitutes a unique feature of this enzyme within the CA family. Areas covered: Starting from a brief description of the main molecular and catalytic features of both enzymes, their role in tumor physiology and their three-dimensional structure, this review describes the main classes of small molecule inhibitors, investigated between 2008 and 2013, able to inhibit these enzymes for both diagnostic and therapeutic applications. Expert opinion: A consistent number of patents on molecules able to inhibit the catalytic activity of CA IX and CA XII have been recently reported. Most patents deal with classical sulfonamide derivatives, demonstrating that introducing suitable substituents on the inhibitor scaffold, good selectivity can be obtained. However, the most impressive results are related to compounds containing novel chemotypes, such as coumarins and thiocumarins. Thus, it is expected that research in next future will be more dedicated to the development of molecules containing new chemotypes and a large number of studies in such field have already been published demonstrating the role of these enzymes in carcinogenesis and metastases formation. © 2013 Informa UK, Ltd.
Anticancer carbonic anhydrase inhibitors: A patent review (2008-2013)
Anticancer carbonic anhydrase inhibitors: A patent review (2008-2013)
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Di Fiore A, De Luca V, Langella E, Nocentini A, Buonanno M, Monti SM, Supuran CT, Capasso C, De Simone G
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Sarnella A, Ferrara Y, Auletta L, Albanese S, Cerchia L, Alterio V, De Simone G, Supuran CT, Zannetti A
* Inhibition of carbonic anhydrases IX/XII by SLC-0111 boosts cisplatin effects in hampering head and neck squamous carcinoma cell growth and invasion (22 views)
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Di Fiore A, Supuran CT, Scaloni A, De Simone G
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Akgül Ö, Lucarini E, Mannelli LDC, Ghelardini C, D'Xambrosio K, Buonanno M, Monti SM, De Simone G, Angeli A, Supuran CT, Carta F
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Pagnozzi D, Pala N, Biosa G, Dallocchio R, Dessì A, Singh PK, Rogolino D, Di Fiore A, De Simone G, Supuran CT, Sechi M
* Interaction Studies between Carbonic Anhydrase and a Sulfonamide Inhibitor by Experimental and Theoretical Approaches (7 views)
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Urbański LJ, Angeli A, Hytönen VP, Di Fiore A, De Simone G, Parkkila S, Supuran CT
* Inhibition of the β-carbonic anhydrase from the protozoan pathogen Trichomonas vaginalis with sulphonamides (148 views)
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Mancuso F, Di Fiore A, De Luca L, Angeli A, De Simone G, Supuran CT, Gitto R
* Design, synthesis and biochemical evaluation of novel carbonic anhydrase inhibitors triggered by structural knowledge on hCA VII (27 views)
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Alterio V, Langella E, Buonanno M, Esposito D, Nocentini A, Berrino E, Bua S, Polentarutti M, Supuran CT, Monti SM, De Simone G
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Mulliri S, Laaksonen A, Spanu P, Farris R, Farci M, Mingoia F, Roviello GN, Mocci F
* Spectroscopic and In Silico Studies on the Interaction of Substituted Pyrazolo[1, 2-a]benzo[1, 2, 3, 4]tetrazine-3-one Derivatives with c-Myc G4-DNA (25 views)
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De Simone G, Bua S, Supuran CT, Alterio V
* Benzyl alcohol inhibits carbonic anhydrases by anchoring to the zinc coordinated water molecule (11 views)
Biochem Biophys Res Commun (ISSN: 0006-291xlinking), 2021 Apr 9; 548: 217-221.
Impact Factor: 3.575
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Langella E, Buonanno M, De Simone G, Monti SM
* Intrinsically disordered features of carbonic anhydrase IX proteoglycan-like domain (30 views)
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Impact Factor: 9.261
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D’ambrosio K, Di Fiore A, Buonanno M, Kumari S, Tiwari M, Supuran CT, Mishra CB, Monti SM, De Simone G
* The crystal structures of 2-(4-benzhydrylpiperazin-1-yl)-N-(4-sulfamoylphenyl)acetamide in complex with human carbonic anhydrase II and VII provide insights into selective CA inhibitor development (84 views)
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Urbański LJ, Di Fiore A, Azizi L, Hytönen VP, Kuuslahti M, Buonanno M, Monti SM, Angeli A, Zolfaghari Emameh R, Supuran CT, De Simone G, Parkkila S
* Biochemical and structural characterisation of a protozoan beta-carbonic anhydrase from Trichomonas vaginalis (125 views)
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Impact Factor: 4.673
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Di Fiore A, Supuran CT, Scaloni A, De Simone G
* Human carbonic anhydrases and post-translational modifications: a hidden world possibly affecting protein properties and functions (122 views)
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Urbański LJ, Angeli A, Hytönen VP, Di Fiore A, Parkkila S, De Simone G, Supuran CT
* Inhibition of the newly discovered β‑carbonic anhydrase from the protozoan pathogen Trichomonas vaginalis with inorganic anions and small molecules (79 views)
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Impact Factor: 3.212
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Sarnella A, D'Avino G, Hill BS, Alterio V, Winum JY, Supuran CT, De Simone G, Zannetti A
* A Novel Inhibitor of Carbonic Anhydrases Prevents Hypoxia-Induced TNBC Cell Plasticity (67 views) (PDF 25 views)
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D'Ambrosio K, Carradori S, Cesa S, Angeli A, Monti SM, Supuran CT, De Simone G
* Catechols: a new class of carbonic anhydrase inhibitors (85 views)
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Angeli A, Carta F, Nocentini A, Winum J, Zalubovskis R, Akdemir A, Onnis V, Eldehna WM, Capasso C, De Simone G, Monti Simona M, Carradori S, Donald WA, Dedhar S, Supuran CT
* Carbonic Anhydrase Inhibitors Targeting Metabolism and Tumor Microenvironment (83 views)
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Bozdag M, Supuran CT, Esposito D, Angeli A, Carta F, Monti SM, De Simone G, Alterio V
* 2-Mercaptobenzoxazoles: a class of carbonic anhydrase inhibitors with a novel binding mode to the enzyme active site (101 views)
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Nocentini A, Alterio V, Bua S, Micheli L, Esposito D, Buonanno M, Bartolucci G, Osman SM, Alothman ZA, Cirilli R, Pierini M, Monti SM, Di Cesare Mannelli L, Gratteri P, Ghelardini C, De Simone G, Supuran CT
* Phenyl(thio)phosphon(amid)ate Benzenesulfonamides as Potent and Selective Inhibitors of Human Carbonic Anhydrases II and VII Counteract Allodynia in a Mouse Model of Oxaliplatin-Induced Neuropathy (111 views)
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Mancuso F, Di Fiore A, De Luca L, Angeli A, Monti SM, De Simone G, Supuran CT, Gitto R
* Looking toward the Rim of the Active Site Cavity of Druggable Human Carbonic Anhydrase Isoforms (109 views)
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Fik-jaskółka MA, Mkrtchyan AF, Saghyan AS, Palumbo R, Belter A, Hayriyan LA, Simonyan H, Roviello V, Roviello GN
* Spectroscopic and SEM evidences for G4-DNA binding by a synthetic alkyne-containing amino acid with anticancer activity (209 views) (PDF 75 views)
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Langella E, Buonanno M, De Simone G, Monti SM
* Intrinsically disordered features of carbonic anhydrase IX proteoglycan-like domain (94 views)
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Alterio V, Kellner M, Esposito D, Liesche-starnecker F, Bua S, Supuran CT, Monti SM, Zeidler R, De Simone G
* Biochemical and structural insights into Carbonic Anhydrase XII/Fab6A10 complex (168 views)
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De Simone G, Di Fiore A, Truppo E, Langella E, Vullo D, Supuran CT, Monti SM
* Exploration of the residues modulating the catalytic features of human carbonic anhydrase XIII by a site-specific mutagenesis approach (222 views)
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Langella E, Alterio V, D'Ambrosio K, Cadoni R, Winum JY, Supuran CT, Monti SM, De Simone G, Di Fiore A
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Buemi MR, Di Fiore A, De Luca L, Angeli A, Mancuso F, Ferro S, Monti SM, Buonanno M, Russo E, De Sarro G, De Simone G, Supuran CT, Gitto R
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De Simone G
* Targeted treatment of anaerobic cancer. Patent evaluation of US2016279084 and US2017056350 (225 views)
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Impact Factor: 3.699
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Alterio V, Esposito D, Monti SM, Supuran CT, De Simone G
* Crystal structure of the human carbonic anhydrase II adduct with 1-(4-sulfamoylphenyl-ethyl)-2, 4, 6-triphenylpyridinium perchlorate, a membrane-impermeant, isoform selective inhibitor (533 views)
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Monti SM, Meccariello A, Ceruso M, Szafranski K, Slawinski J, Supuran CT
* Inhibition studies of Brucella suis beta-carbonic anhydrases with a series of 4-substituted pyridine-3-sulphonamides (369 views)
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Angeli A, Buonanno M, Donald WA, Monti SM, Supuran CT
* The zinc - but not cadmium - containing zeta-carbonic from the diatom Thalassiosira weissflogii is potently activated by amines and amino acids (279 views)
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Impact Factor: 3.929
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De Simone G, Angeli A, Bozdag M, Supuran CT, Winum JY, Monti SM, Alterio V
* Inhibition of carbonic anhydrases by a substrate analog: benzyl carbamate directly coordinates the catalytic zinc ion mimicking bicarbonate binding (243 views)
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Impact Factor: 6.169
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Langella E, Buonanno M, Vullo D, Dathan N, Leone M, Supuran C, De Simone G, Monti SM
* Biochemical, biophysical and molecular dynamics studies on the proteoglycan-like domain of carbonic anhydrase IX (317 views)
Cell Mol Life Sci (ISSN: 1420-682xlinking), 2018 Sep; 75(17): 3283-3296.
Impact Factor: 6.721
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Supuran CT, Alterio V, Di Fiore A, D'Ambrosio K, Carta F, Monti SM, De Simone G
* Inhibition of carbonic anhydrase IX targets primary tumors, metastases, and cancer stem cells: Three for the price of one (532 views)
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Impact Factor: 8.29
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Mishra CB, Kumari S, Angeli A, Bua S, Buonanno M, Monti SM, Tiwari M, Supuran CT
* Discovery of potent anti-convulsant carbonic anhydrase inhibitors: Design, synthesis, in vitro and in vivo appraisal (234 views)
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Impact Factor: 4.816
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Di Fiore A, Monti DM, Scaloni A, De Simone G, Monti SM
* Protective Role of Carbonic Anhydrases III and VII in Cellular Defense Mechanisms upon Redox Unbalance (214 views)
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Impact Factor: 4.936
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Buonanno M, Di Fiore A, Langella E, D’ambrosio K, Supuran CT, Monti SM, De Simone G
* The Crystal Structure of a hCA VII Variant Provides Insights into the Molecular Determinants Responsible for Its Catalytic Behavior (303 views)
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Impact Factor: 3.687
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D'Ambrosio K, Supuran CT, De Simone G
* Are Carbonic Anhydrases Suitable Targets to Fight Protozoan Parasitic Diseases? (250 views)
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Impact Factor: 4.63
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De Simone G, Langella E, Esposito D, Supuran CT, Monti SM, Winum JY, Alterio V
* Insights into the binding mode of sulphamates and sulphamides to hCA II: crystallographic studies and binding free energy calculations (251 views)
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Impact Factor: 3.638
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Monti DM, De Simone G, Langella E, Supuran CT, Di Fiore A, Monti SM
* Insights into the role of reactive sulfhydryl groups of Carbonic Anhydrase III and VII during oxidative damage (354 views)
J Enzym Inhib Med Ch (ISSN: 1475-6366, 1475-6374electronic, 1475-6366linking), 2017 Dec; 32(1): 5-12.
Impact Factor: 3.638
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Marchiori MF, Riul TB, Oliveira Bortot L, Andrade P, Junqueira GG, Foca G, Doti N, Ruvo M, Dias-baruffi M, Carvalho I, Campo VL
* Binding of triazole-linked galactosyl arylsulfonamides to galectin-3 affects Trypanosoma cruzi cell invasion (1018 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 0968-0896linking), 2017 Nov 1; 25(21): 6049-6059.
Impact Factor: 2.881
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Brunò E, Buemi MR, Di Fiore A, De LucaL, Ferro S, Angeli A, Cirilli R, Sadutto D, Alterio V, Monti SM, Supuran CT, De Simone G, Gitto R
* Probing Molecular Interactions between Human Carbonic Anhydrases (hCAs) and a Novel Class of Benzenesulfonamides (385 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2017 May 25; 60(10): 4316-4326.
Impact Factor: 6.253
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Buonanno M, Langella E, Zambrano N, Succoio M, Sasso E, Alterio V, Di Fiore A, Sandomenico A, Supuran CT, Scaloni A, Monti SM, De Simone G
* Disclosing the Interaction of Carbonic Anhydrase IX with Cullin-Associated NEDD8-Dissociated Protein 1 by Molecular Modeling and Integrated Binding Measurements (279 views)
Acs Chem Biol (ISSN: 1554-8929), 2017 Apr 19; N/D: N/D-N/D.
Impact Factor: 4.592
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Mishra CB, Kumari S, Angeli A, Monti SM, Buonanno M, Tiwari M, Supuran CT
* Discovery of Benzenesulfonamides with Potent Human Carbonic Anhydrase Inhibitory and Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Assessment (829 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2017 Mar 23; 60(6): 2456-2469.
Impact Factor: 6.253
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Altug C, Gunes H, Nocentini A, Monti SM, Buonanno M, Supuran CT
* Synthesis of isoxazole-containing sulfonamides with potent carbonic anhydrase II and VII inhibitory properties (301 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 0968-0896linking), 2017 Feb 15; 25(4): 1456-1464.
Impact Factor: 2.881
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Angapelly S, Ramya PV, Angeli A, Monti SM, Buonanno M, Alvala M, Supuran CT, Arifuddin M
* Discovery of 4-sulfamoyl-phenyl-beta-lactams as a new class of potent carbonic anhydrase isoforms I, II, IV and VII inhibitors: The first example of subnanomolar CA IV inhibitors (304 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 0968-0896linking), 2017 Jan 15; pii:S0968-0896(16): 539-544.
Impact Factor: 2.881
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Martínez-fernández L, Granucci G, Pollum M, Crespo-hernández CE, Persico M, Corral I
* Decoding the Molecular Basis for the Population Mechanism of the Triplet Phototoxic Precursors in UVA Light-Activated Pyrimidine Anticancer Drugs (363 views)
Chemistry (ISSN: 0947-6539, 1521-3765, 1521-3765electronic), 2017; 23(11): 2619-2627.
Impact Factor: 5.16
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Angapelly S, Ramya PVS, Angeli A, Monti SM, Buonanno M, Alvala M, Supuran CT, Arifuddin M
* Discovery of 4-sulfamoyl-phenyl-β-lactams as a new class of potent carbonic anhydrase isoforms I, II, IV and VII inhibitors: The first example of subnanomolar CA IV inhibitors (255 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 0968-0896linking), 2017; 25(2): 539-544.
Impact Factor: 2.881
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Alterio V, Cadoni R, Esposito D, Vullo D, Fiore AD, Monti SM, Caporale A, Ruvo M, Sechi M, Dumy P, Supuran CT, De Simone G, Winum JY
* Benzoxaborole as a new chemotype for carbonic anhydrase inhibition (434 views)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2016 Sep 29; 52(80): 11983-11986.
Impact Factor: 6.319
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Vullo D, Supuran CT, Scozzafava A, De Simone G, Monti SM, Alterio V, Carta F
* Kinetic and X-ray crystallographic investigations of substituted 2-thio-6-oxo-1, 6-dihydropyrimidine-benzenesulfonamides acting as carbonic anhydrase inhibitors (254 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 0968-0896linking), 2016 Aug 15; 24(16): 3643-3648.
Impact Factor: 2.93
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Di Fiore A, De Simone G, Alterio V, Riccio V, Winum JY, Carta F, Supuran CT
* The anticonvulsant sulfamide JNJ-26990990 and its S, S-dioxide analog strongly inhibit carbonic anhydrases: solution and X-ray crystallographic studies (249 views)
Org Biomol Chem (ISSN: 1477-0520, 1477-0539, 1477-0539electronic), 2016 Jun 07; 14(21): 4853-4858.
Impact Factor: 3.564
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Del Prete S, De Luca V, De Simone G, Supuran CT, Capasso C
* Cloning, expression and purification of the complete domain of the eta-carbonic anhydrase from Plasmodium falciparum (352 views)
J Enzym Inhib Med Ch (ISSN: 1475-6366, 1475-6374electronic, 1475-6366linking), 2016 Jun; 31(sup4): 54-59.
Impact Factor: 4.293
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Langella E, D'Ambrosio K, D'Ascenzio M, Carradori S, Monti SM, Supuran CT, De Simone G
* A Combined Crystallographic and Theoretical Study Explains the Capability of Carboxylic Acids to Adopt Multiple Binding Modes in the Active Site of Carbonic Anhydrases (335 views)
Chemistry (ISSN: 0947-6539, 1521-3765, 1521-3765electronic), 2016 Jan 4; 22(1): 97-100.
Impact Factor: 5.317
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Mishra CB, Kumari S, Angeli A, Monti SM, Buonanno M, Prakash A, Tiwari M, Supuran CT
* Design, synthesis and biological evaluation of N-(5-methyl-isoxazol-3-yl/1, 3, 4-thiadiazol-2-yl)-4-(3-substitutedphenylureido) benzenesulfonamides as human carbonic anhydrase isoenzymes I, II, VII and XII inhibitors (292 views)
J Enzyme Inhib Med Chem, 2016; 17: 1-6.
Impact Factor: 3.428
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Mollica A, Locatelli M, Macedonio G, Carradori S, Sobolev AP, De Salvador RF, Monti SM, Buonanno M, Zengin G, Angeli A, Supuran CT
* Microwave-assisted extraction, HPLC analysis, and inhibitory effects on carbonic anhydrase I, II, VA, and VII isoforms of 14 blueberry Italian cultivars (242 views)
J Enzyme Inhib Med Chem, 2016; 31(sup4): N/D-N/D.
Impact Factor: 3.428
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La Regina G, Coluccia A, Famiglini V, Pelliccia S, Monti L, Vullo D, Nuti E, Alterio V, De Simone G, Monti SM, Pan P, Parkkila S, Supuran CT, Rossello A, Silvestri R
* Discovery of 1, 1'-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors (335 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2015 Nov 12; 58(21): 8564-8572.
Impact Factor: 5.589
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Di Fiore A, Vergara A, Caterino M, Alterio V, Monti SM, Ombouma J, Dumy P, Vullo D, Supuran CT, Winum JY, De Simone G
* Hydroxylamine-O-sulfonamide is a versatile lead compound for the development of carbonic anhydrase inhibitors (320 views) (PDF 223 views)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2015 Jul 2; 51(57): 11519-11522.
Impact Factor: 6.567
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De Simone G, Monti SM, Alterio V, Buonanno M, De Luca V, Rossi M, Carginale V, Supuran CT, Capasso C, Di Fiore A
* Crystal structure of the most catalytically effective carbonic anhydrase enzyme known, SazCA from the thermophilic bacterium Sulfurihydrogenibium azorense (304 views)
Bioorg Med Chem Lett (ISSN: 0960-894x), 2015 May 1; 25(9): 2002-2006.
Impact Factor: 2.486
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Alterio V, Tanc M, Ivanova J, Zalubovskis R, Vozny I, Monti SM, Di Fiore A, De Simone G, Supuran CT
* X-ray crystallographic and kinetic investigations of 6-sulfamoyl-saccharin as a carbonic anhydrase inhibitor (344 views)
Org Biomol Chem (ISSN: 1477-0520, 1477-0539, 1477-0539electronic), 2015 Apr 7; 13(13): 4064-4069.
Impact Factor: 3.559
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De Simone G, Di Fiore A, Capasso C, Supuran CT
* The zinc coordination pattern in the eta-carbonic anhydrase from Plasmodium falciparum is different from all other carbonic anhydrase genetic families (471 views)
Bioorg Med Chem Lett (ISSN: 0960-894x), 2015 Apr 1; 25(7): 1385-1389.
Impact Factor: 2.486
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Alterio V, Langella E, De Simone G, Monti SM
* Cadmium-containing carbonic anhydrase CDCA1 in marine diatom Thalassiosira weissflogii (630 views)
Mar Drugs (ISSN: 1660-3397, 1660-3397linking), 2015 Mar 25; 13(4): 1688-1697.
Impact Factor: 3.345
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Monti SM, Supuran CT, De Simone G
* DPP-4 inhibitors: a patent review (2012 - 2014) (573 views)
Expert Opin Ther Pat (ISSN: 1354-3776, 1744-7674electronic), 2015 Feb; 25(2): 209-236.
Impact Factor: 4.626
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Supuran CT, Capasso C, De Simone G
* Carbonic Anhydrase II as Target for Drug Design (262 views)
Carbonic Anhydrases As Biocatalysts, 2015 Jan 08; N/D: 51-90.
Impact Factor: 0
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Monti SM, Supuran CT, De Simone G, Di Fiore A
* Carbonic Anhydrase VII (215 views)
Carbonic Anhydrases As Biocatalysts, 2015 Jan 08; N/D: 151-168.
Impact Factor: 0
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Supuran CT, De Simone G
Carbonic Anhydrases: An Overview (234 views)
Carbonic Anhydrases As Biocatalysts, 2015 Jan 08; N/D: 3-13.
Impact Factor: 0
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D'Ambrosio K, De Simone G, Supuran CT
* Human Carbonic Anhydrases: Catalytic Properties, Structural Features, and Tissue Distribution (281 views)
Carbonic Anhydrases As Biocatalysts, 2015 Jan 08; N/D: 17-30.
Impact Factor: 0
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D'Ambrosio K, Carradori S, Monti SM, Buonanno M, Secci D, Vullo D, Supuran CT, De Simone G
* Out of the active site binding pocket for carbonic anhydrase inhibitors (406 views) (PDF 237 views)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2015 Jan 7; 51(2): 302-305.
Impact Factor: 6.567
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Ceruso M, Carta F, Osman SM, Alothman Z, Monti SM, Supuran CT
* Inhibition studies of bacterial, fungal and protozoan β-class carbonic anhydrases with Schiff bases incorporating sulfonamide moieties (367 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 0968-0896linking), 2015; 23(15): 4181-4187.
Impact Factor: 2.923
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Iqbal J, Al-rashida M, Durdagi S, Alterio V, Di Fiore A
* Recent developments of carbonic anhydrase inhibitors as potential drugs (423 views)
Biomed Res Int (ISSN: 2314-6133, 2314-6141), 2015; 2015: 174178-174178.
Impact Factor: 2.134
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Di Fiore A, Alterio V, Monti SM, De Simone G, D’Ambrosio K
* Thermostable carbonic anhydrases in biotechnological applications (487 views)
Int J Mol Sc (ISSN: 1422-0067, 1661-6596, 1422-0067linking), 2015; 16(7): 15456-15480.
Impact Factor: 3.257
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Dathan NA, Alterio V, Troiano E, Vullo D, Ludwig M, De Simone G, Supuran CT, Monti SM
* Biochemical Characterization Of The Chloroplastic β-Carbonic Anhydrase From Flaveria Bidentis (l. ) "kuntze" (449 views)
J Enzym Inhib Med Ch (ISSN: 1475-6366, 1475-6374electronic, 1475-6366linking), 2014; 29(4): 500-504.
Impact Factor: 2.332
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De Simone G, Pizika G, Monti SM, Di Fiore A, Ivanova J, Vozny I, Trapencieris P, Zalubovskis R, Supuran CT, Alterio V
* Hydrophobic substituents of the phenylmethylsulfamide moiety can be used for the development of new selective carbonic anhydrase inhibitors (341 views)
Biomed Res Int (ISSN: 2314-6133, 2314-6141), 2014; 2014: 523210-523210.
Impact Factor: 1.579
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Alterio V, Pan P, Parkkila S, Buonanno M, Supuran CT, Monti SM, De Simone G
* The Structural Comparison Between Membrane-Associated Human Carbonic Anhydrases Provides Insights Into Drug Design Of Selective Inhibitors (416 views)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 2014; 101(7): 769-778.
Impact Factor: 2.385
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Alterio V, Monti SM, De Simone G
* Thermal-stable carbonic anhydrases: a structural overview (389 views)
Subcell Biochem (ISSN: 0306-0225), 2014; 75: 387-404.
Impact Factor: 33.116
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Rami M, Dubois L, Parvathaneni NK, Alterio V, van Kuijk SJ, Monti SM, Lambin P, De Simone G, Supuran CT, Winum JY
* Hypoxia-targeting carbonic anhydrase IX inhibitors by a new series of nitroimidazole-sulfonamides/sulfamides/sulfamates (546 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2013 Nov 14; 56(21): 8512-8520.
Impact Factor: 5.48
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De Simone G, Alterio V, Supuran CT
* Exploiting the hydrophobic and hydrophilic binding sites for designing carbonic anhydrase inhibitors (507 views)
Expert Opin Drug Discov (ISSN: 1746-0441), 2013 Jul; 8(7): 793-810.
Impact Factor: 3.467
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Di Fiore A, Capasso C, De Luca V, Monti SM, Carginale V, Supuran CT, Scozzafava A, Pedone C, Rossi M, De Simone G
* X-ray structure of the first 'extremo-alpha-carbonic anhydrase', a dimeric enzyme from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 (515 views)
Acta Crystallogr D Biol Crystallogr (ISSN: 0907-4449, 0907-4449linking), 2013 Jun; 69(6): 1150-1159.
Impact Factor: 7.232
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Monti SM, De Simone G, Dathan NA, Ludwig M, Vullo D, Scozzafava A, Capasso C, Supuran CT
* Kinetic And Anion Inhibition Studies Of A Beta-Carbonic Anhydrase (fbica 1) From The C-4 Plant Flaveria Bidentis (440 views)
Bioorg Med Chem Lett (ISSN: 0960-894x), 2013 Mar 15; 23(6): 1626-1630.
Impact Factor: 2.331
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Buanne P, Renzone G, Monteleone F, Vitale M, Monti SM, Sandomenico A, Garbi C, Montanaro D, Accardo M, Troncone G, Zatovicova M, Csaderova L, Supuran CT, Pastorekova S, Scaloni A, De Simone G, Zambrano N
* Characterization of carbonic anhydrase ix interactome reveals proteins assisting its nuclear localization in hypoxic cells (393 views)
J Proteome Res (ISSN: 1535-3893), 2013 Jan; 12(1): 282-292.
Impact Factor: 5.001
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Del Giudice R, Monti DM, Truppo E, Arciello A, Supuran CT, De Simone G, Monti SM
* Human Carbonic Anhydrase Vii Protects Cells From Oxidative Damage (366 views)
Biol Chem Biological Chemistry (ISSN: 1431-6730, 1431-1673, 1437-4315), 2013; 394(10): 1343-1348.
Impact Factor: 2.689
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Alterio V, Di Fiore A, D'Ambrosio K, Supuran CT, De Simone G
* Multiple binding modes of inhibitors to carbonic anhydrases: How to design specific drugs targeting 15 different isoforms? (452 views)
Chem Rev (ISSN: 0009-2665), 2012 Sep; 112(8): 4421-4468.
Impact Factor: 41.298
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De Simone G, Supuran CT
* (In)organic anions as carbonic anhydrase inhibitors (379 views)
J Chem Res (ISSN: 0162-0134, 1873-3344, 0162-0134print), 2012 Jun; 111: 117-129.
Impact Factor: 3.197
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Alterio V, Langella E, Viparelli F, Vullo D, Ascione G, Dathan NA, Morel FM, Supuran CT, De Simone G, Monti SM
* Structural and inhibition insights into carbonic anhydrase CDCA1 from the marine diatom Thalassiosira weissflogii (435 views)
Biochimie (ISSN: 0300-9084, 1638-6183, 1638-6183electronic), 2012 May; 94(5): 1232-1241.
Impact Factor: 3.142
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Zannetti A, Iommelli F, Speranza A, Salvatore M, Del Vecchio S
* 3'-deoxy-3'-18F-fluorothymidine (FLT) PET/CT to guide therapy with epidermal growth factor receptor (EGFR) antagonists and Bcl-xL inhibitors in non-small cell lung cancer (614 views)
J Nucl Med (ISSN: 0161-5505, 1535-5667, 1535-5667electronic), 2012 Mar 1; 53(3): 443-450.
Impact Factor: 5.774
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Zannetti A, Iommelli F, Speranza A, Salvatore M, Del Vecchio S
* 3'-deoxy-3'-18F-fluorothymidine PET/CT to guide therapy with epidermal growth factor receptor antagonists and Bcl-xL inhibitors in non-small cell lung cancer (525 views)
J Nucl Med (ISSN: 1535-5667, 0161-5505, 1535-5667electronic), 2012 Mar 1; 53(3): 443-450.
Impact Factor: 5.774
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Truppo E, Supuran CT, Sandomenico A, Vullo D, Innocenti A, Di Fiore A, Alterio V, De Simone G, Monti SM
* Carbonic anhydrase VII is S-glutathionylated without loss of catalytic activity and affinity for sulfonamide inhibitors (384 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2012 Feb 15; 22(4): 1560-1564.
Impact Factor: 2.338
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Monti SM, Supuran CT, De Simone G
* Carbonic anhydrase IX as a target for designing novel anticancer drugs (526 views)
Curr Med Chem (ISSN: 0929-8673, 1875-533x, 1875-533xelectronic), 2012 Feb; 19(6): 821-830.
Impact Factor: 4.07
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De Simone G
* Editorial: Zinc Metallo-Enzymes As Target For Drug Design (423 views)
Curr Med Chem (ISSN: 0929-8673, 1875-533x, 1875-533xelectronic), 2012 Feb; 19(6): 820-1012.
Impact Factor: 4.07
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Monti SM, Maresca A, Viparelli F, Carta F, De Simone G, Muehlschlegel FA, Scozzafava A, Supuran CT
* Dithiocarbamates are strong inhibitors of the beta-class fungal carbonic anhydrases from Cryptococcus neoformans, Candida albicans and Candida glabrata (392 views)
Bioorg Med Chem Lett (ISSN: 0960-894x), 2012 Jan 15; 22(2): 859-862.
Impact Factor: 2.338
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D'Ambrosio K, Smaine F-Z, Carta F, De Simone G, Winum J-Y, Supuran CT
* Development of potent carbonic anhydrase inhibitors incorporating both sulfonamide and sulfamide groups (467 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2012; 55(15): 6776-6783.
Impact Factor: 5.614
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Sorriento D, Santulli G, Del Giudice C, Anastasio A, Trimarco B, Iaccarino G
* Endothelial cells are able to synthesize and release catecholamines both in vitro and in vivo (423 views)
Hypertensionhypertension (ISSN: 0194-911x), 2012; 60(1): 129-136.
Impact Factor: 6.873
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Di Fiore A, Maresca A, Supuran CT, De Simone G
* Hydroxamate represents a versatile zinc binding group for the development of new carbonic anhydrase inhibitors (361 views)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2012; 48(70): 8838-8840.
Impact Factor: 6.378
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Caraci F, Molinaro G, Battaglia G, Giuffrida ML, Riozzi B, Traficante A, Bruno V, Cannella M, Merlo S, Wang X, Heinz BA, Nisenbaum ES, Britton TC, Drago F, Sortino MA, Copani A, Nicoletti F
* Targeting group II Metabotropic Glutamate (mGlu) receptors for the treatment of psychosis associated with alzheimer's disease: Selective activation of mGlu2 receptors amplifies β-amyloid toxicity in cultured neurons, whereas dual activation of mGlu2 and mGlu3 receptors is neuroprotective (748 views)
Mol Pharmacol (ISSN: 0026-895x), 2011 Mar; 79(3): 618-626.
Impact Factor: 4.883
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Di Fiore A, Maresca A, Alterio V, Supuran CT, De Simone G
* Carbonic anhydrase inhibitors: X-ray crystallographic studies for the binding of N-substituted benzenesulfonamides to human isoform II (338 views)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2011; 47(42): 11636-11638.
Impact Factor: 6.169
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Viparelli F, Monti SM, De Simone G, Innocenti A, Scozzafava A, Xu Y, Morel FMM, Supuran CT
* Inhibition Of The R1 Fragment Of The Cadmium-Containing Zeta-Class Carbonic Anhydrase From The Diatom Thalassiosira Weissflogii With Anions (333 views)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2010 Sep 15; 20(16): 4745-4748.
Impact Factor: 2.661
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Alterio V, Monti SM, Truppo E, Pedone C, Supuran CT, De Simone G
* The first example of a significant active site conformational rearrangement in a carbonic anhydrase-inhibitor adduct: The carbonic anhydrase I-topiramate complex (446 views)
Org Biomol Chem (ISSN: 1477-0520, 1477-0539, 1477-0539electronic), 2010 Sep 7; 8(15): 3528-3533.
Impact Factor: 3.451
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Di Fiore A, Truppo E, Supuran CT, Alterio V, Dathan N, Bootorabi F, Parkkila S, Monti SM, De Simone G
* Crystal structure of the C183S/C217S mutant of human CA VII in complex with acetazolamide (325 views)
Bioorg Med Chem Lett (ISSN: 0960-894x), 2010 Sep 1; 20(17): 5023-5026.
Impact Factor: 2.661
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Di Fiore A, Monti SM, Innocenti A, Winum J-Y, De Simone G, Supuran CT
* Carbonic anhydrase inhibitors: Crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV (352 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2010 Jun 15; 20(12): 3601-3605.
Impact Factor: 2.661
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De Simone G, Supuran CT
* Carbonic anhydrase IX: Biochemical and crystallographic characterization of a novel antitumor target (398 views)
Bba-Gen Subjects (ISSN: 1570-9639, 0006-3002, 0925-4439), 2010 Feb; 1804(2): 404-409.
Impact Factor: 2.773
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Guler OO, De Simone G, Supuran CT
* Drug design studies of the novel antitumor targets carbonic anhydrase IX and XII (540 views)
Curr Med Chem (ISSN: 0929-8673, 1875-533x, 1875-533xelectronic), 2010; 17(15): 1516-1526.
Impact Factor: 4.63
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Supuran CT, Di Fiore A, Alterio V, Monti SM, De Simone G
* Recent advances in structural studies of the carbonic anhydrase family: The crystal structure of human CA IX and CA XIII (471 views)
Curr Pharm Des Current Pharmaceutical Design (ISSN: 1381-6128, 1873-4286), 2010; 16(29): 3246-3254.
Impact Factor: 4.774
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Innocenti A, Pastorekova S, Pastorek J, Scozzafava A, De Simone G, Supuran CT
* The proteoglycan region of the tumor-associated carbonic anhydrase isoform IX acts as anintrinsic buffer optimizing CO2 hydration at acidic pH values characteristic of solid tumors (264 views)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2009 Oct 15; 19(20): 5825-5828.
Impact Factor: 2.65
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Vitale RM, Alterio V, Innocenti A, Winum JY, Monti SM, De Simone G, Supuran CT
* Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis- sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors (462 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2009 Oct 8; 52(19): 5990-5998.
Impact Factor: 4.802
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Alterio V, Hilvo M, Di Fiore A, Supuran CT, Pan P, Parkkila S, Scaloni A, Pastorek J, Pastorekova S, Pedone C, Scozzafava A, Monti SM, De Simone G
* Crystal structure of the catalytic domain of the tumor-associated human carbonic anhydrase IX (571 views)
P Natl Acad Sci Usa (ISSN: 0027-8424, 1091-6490, 0027-8424print), 2009 Sep 22; 106(38): 16233-16238.
Impact Factor: 9.432
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De Simone G, Scozzafava A, Supuran CT
* Which Carbonic Anhydrases are Targeted by the Antiepileptic Sulfonamides and Sulfamates? (352 views)
Chem Biol Drug Des (ISSN: 1747-0277, 1747-0285), 2009 Sep; 74(3): 317-321.
Impact Factor: 2.473
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Di Fiore A, Monti SM, Hilvo M, Parkkila S, Romano V, Scaloni A, Pedone C, Scozzafava A, Supuran CT, De Simone G
* Crystal structure of human carbonic anhydrase XIII and its complex with the inhibitor acetazolamide (542 views)
Proteins (ISSN: 1097-0134, 0887-3585, 1097-0134electronic), 2009 Jan; 74(1): 164-175.
Impact Factor: 3.085
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Hilvo M, De Simone G, Supuran CT, Parkkila S
* Advances in the Inhibitory and Structural Investigations on Carbonic Anhydrase Isozymes XIII and XV (289 views)
Drug Des Of Zinc Enzyme Inhibitors (ISSN: 9780-4702, 9780-470275009), 2009; N/D: 273-283.
Impact Factor: 1.156
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De Simone G, Supuran CT
* Drug Design of Antiobesity Carbonic Anhydrase Inhibitors (332 views)
Drug Des Of Zinc Enzyme Inhibitors (ISSN: 9780-4702, 9780-470275009), 2009; 66(DECEMBERSPEC.I): 241-254.
Impact Factor: 1.156
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Alterio V, Di Fiore A, D'Ambrosio K, Supuran CT, De Simone G
* X-Ray Crystallography of Carbonic Anhydrase Inhibitors and Its Importance in Drug Design (426 views)
Drug Des Of Zinc Enzyme Inhibitors (ISSN: 9780-4702, 9780-470275009), 2009; N/D: 73-138.
Impact Factor: 1.156
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Hilvo M, Baranauskiene L, Salzano AM, Scaloni A, Matulis D, Innocenti A, Scozzafava A, Monti SM, Di Fiore A, De Simone G, Lindfors M, Janis J, Valjakka J, Pastorekova S, Pastorek J, Kulomaa MS, Nordlund HR, Supuran CT, Parkkila S
* Biochemical characterization of CA IX, one of the most active carbonic anhydrase isozymes (459 views)
Jbc Papers (ISSN: 0021-9258, 1083-351x, 0021-9258linking), 2008 Oct 10; 283(41): 27799-27809.
Impact Factor: 5.52
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D'Ambrosio K, Vitale R, Dogne J, Masereel B, Innocenti A, Scozzafava A, De Simone G, Supuran CT
* Ccarbonic Anhydrase Inhibitors: Bioreductive Nitro-Containing Sulfonamides With Selectivity For Targeting The Tumor Associated Isoforms Ix And Xii (823 views)
J Med Chem (ISSN: 1520-4804, 0022-2623, 0022-2623print), 2008 Jun 12; 51(11): 3230-3237.
Impact Factor: 4.898
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Supuran CT, Di Fiore A, De Simone G
* Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity (560 views)
Expert Opin Emerg Drugsexpert Opinion On Emerging Drugs (ISSN: 1472-8214), 2008 Jun; 13(2): 383-392.
Impact Factor: 3.08
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Di Fiore A, Pedone C, Antel J, Waldeck H, Witte A, Wurl M, Scozzafava A, Supuran CT, De Simone G
* Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors (385 views)
Bioorg Med Chem Lett (ISSN: 1464-3405, 0960-894x, 1464-3405electronic), 2008 Apr 15; 18(8): 2669-2674.
Impact Factor: 2.531
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Innocenti A, Scozzafava A, Parkkila S, Puccetti L, De Simone G, Supuran CT
* Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates (360 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2008 Apr 1; 18(7): 2267-2271.
Impact Factor: 2.531
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Leese MP, Jourdan FL, Gaukroger K, Mahon MF, Newman SP, Foster PA, Stengel C, Regis-Lydi S, Ferrandis E, Di Fiore A, De Simone G, Supuran CT, Purohit A, Reed MJ, Potter BVL
* Structure-activity relationships of C-17 cyano-substituted estratrienes as anticancer agents (462 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2008 Mar 13; 51(5): 1295-1308.
Impact Factor: 4.898
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De Simone G, Di Fiore A, Supuran CT
* Are carbonic anhydrase inhibitors suitable for obtaining antiobesity drugs? (472 views)
Curr Pharm Des Current Pharmaceutical Design (ISSN: 1381-6128, 1873-4286), 2008 Mar; 14(7): 655-660.
Impact Factor: 4.399
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D'Ambrosio K, Masereel B, Thiry A, Scozzafava A, Supuran CT, De Simone G
* Carbonic anhydrase inhibitors: Binding of indanesulfonamides to the human isoform II (378 views)
Chemmedchem (ISSN: 1860-7179, 1860-7187, 1860-7187electronic), 2008 Mar; 3(3): 473-477.
Impact Factor: 3.15
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Supuran CT, De Simone G
Carbonic anhydrases--an overview (354 views)
Curr Pharm Des, 2008; 14(7): 603-614.
Impact Factor: 0
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Hilvo M, Innocenti A, Monti SM, De Simone G, Supuran CT, Parkkila S
* Recent advances in research on the most novel carbonic anhydrases, CA XIII and XV (479 views)
Curr Pharm Des Current Pharmaceutical Design (ISSN: 1381-6128, 1873-4286), 2008; 14(7): 672-678.
Impact Factor: 4.399
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Alterio V, De Simone G, Monti SM, Scozzafava A, Supuran CT
* Carbonic anhydrase inhibitors: Inhibition of human, bacterial, and archaeal isozymes with benzene-1, 3-disulfonamides-Solution and crystallographic studies (329 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2007 Sep 1; 17(15): 4201-4207.
Impact Factor: 2.604
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Vitale RM, Pedone C, Amodeo P, Antel J, Wurl M, Scozzafava A, Supuran CT, De Simone G
* Molecular modeling study for the binding of zonisamide and topiramate to the human mitochondrial carbonic anhydrase isoform VA (335 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 1464-3391electronic), 2007 Jun 15; 15(12): 4152-4158.
Impact Factor: 2.662
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Di Fiore A, Scozzafava A, Winum JY, Montero JL, Pedone C, Supuran CT, De Simone G
* Carbonic anhydrase inhibitors: binding of an antiglaucoma glycosyl-sulfanilamide derivative to human isoform II and its consequences for the drug design of enzyme inhibitors incorporating sugar moieties (410 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2007 Mar 15; 17(6): 1726-1731.
Impact Factor: 2.604
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De Simone G, Supuran CT
* Antiobesity carbonic anhydrase inhibitors (474 views)
Curr Top Med Chem (ISSN: 1568-0266, 1568-0266linking, 1873-4294electronic), 2007; 7(9): 879-884.
Impact Factor: 4.325
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Leese MP, Leblond B, Smith A, Newman SP, Di Fiore A, De Simone G, Supuran CT, Purohit A, Reed MJ, Potter BVL
* 2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity (931 views)
J Med Chem (ISSN: 0022-2623print, 0022-2623linking, 1520-4804), 2006 Dec 28; 49(26): 7683-7696.
Impact Factor: 5.115
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Menchise V, De Simone G, Di Fiore A, Scozzafava A, Supuran CT
* Carbonic anhydrase inhibitors: X-ray crystallographic studies for the binding of 5-amino-1, 3, 4-thiadiazole-2-sulfonamide and 5-(4-amino-3-chloro-5-fluorophenylsulfonamido)1, 3, 4-thiadiazole-2-sulfon amide to human isoform II (310 views)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2006 Dec 15; 16(24): 6204-6208.
Impact Factor: 2.538
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De Simone G, Vitale RM, Di Fiore A, Pedone C, Scozzafava A, Montero JL, Winum JY, Supuran CT
* Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX (474 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2006 Sep 7; 49(18): 5544-5551.
Impact Factor: 5.115
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Alterio V, Vitale RM, Monti SM, Pedone C, Scozzafava A, Cecchi A, De Simone G, Supuran CT
* Carbonic anhydrase inhibitors: X-ray and molecular modeling study for the interaction of a fluorescent antitumor sulfonamide with isozyme II and IX (484 views)
J Am Chem Soc (ISSN: 0002-7863, 0002-2786, 1520-5126), 2006 Jun 28; 128(25): 8329-8335.
Impact Factor: 7.696
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Di Fiore A, Pedone C, D'Ambrosio K, Scozzafava A, De Simone G, Supuran CT
* Carbonic anhydrase inhibitors: Valdecoxib binds to a different active site region of the human isoform II as compared to the structurally related cyclooxygenase II 'selective' inhibitor celecoxib (323 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2006 Jan 15; 16(2): 437-442.
Impact Factor: 2.538
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Grasso G, D'Agata R, Rizzarelli E, Spoto G, D'Andrea LD, Pedone C, Picardi A, Romanelli A, Fragai M, Yeo KJ
* Activity of anchored human matrix metalloproteinase-1 catalytic domain on Au(111) surfaces monitored by ESI-MS (575 views)
J Mass Spectrom (ISSN: 1076-5174, 1096-9888), 2005 Dec; 40(12): 1565-1571.
Impact Factor: 3.574
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De Luca S, Della Moglie R, De Capua A, Morelli G
* New synthetic strategy for o-NBS protected amino acids and their use in synthesis of mono-benzylated peptides (447 views)
Tetrahedron Lett (ISSN: 0040-4039), 2005 Sep 26; 46(39): 6637-6640.
Impact Factor: 2.477
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Menchise V, De Simone G, Alterio V, Di Fiore A, Pedone C, Scozzafava A, Supuran CT
* Carbonic anhydrase inhibitors: Stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide complexed with isozyme II (482 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2005 Sep 8; 48(18): 5721-5727.
Impact Factor: 4.926
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De Simone G, Di Fiore A, Menchise V, Pedone C, Antel J, Casini A, Scozzafava A, Wurl M, Supuran CT
* Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studies (420 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2005 May 2; 15(9): 2315-2320.
Impact Factor: 2.478
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Di Fiore A, De Simone G, Menchise V, Pedone C, Casini A, Scozzafava A, Supuran CT
* Carbonic anhydrase inhibitors: X-ray crystal structure of a benzenesulfonamide strong CA II and CA IX inhibitor bearing a pentafluorophenylaminothioureido tail in complex with isozyme II (489 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2005 Apr 1; 15(7): 1937-1942.
Impact Factor: 2.478
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Fonti R, Latella G, Caprilli R, Frieri G, Marcheggiano A, Sambuy Y
Carbonic anhydrase I reduction in colonic mucosa of patients with active ulcerative colitis (432 views)
Digestive Diseases And Sciences (ISSN: 0163-2116), 1998; 43(9): 2086-2092.
Impact Factor: 1.972
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* Biochemical, structural, and computational studies of a γ-carbonic anhydrase from the pathogenic bacterium Burkholderia pseudomallei (10 views)
Comput Struct Biotechnol J (ISSN: 2001-0370linking), 2022 Jul 27; 20: 4185-4194.
Impact Factor: 6.155
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Sarnella A, Ferrara Y, Auletta L, Albanese S, Cerchia L, Alterio V, De Simone G, Supuran CT, Zannetti A
* Inhibition of carbonic anhydrases IX/XII by SLC-0111 boosts cisplatin effects in hampering head and neck squamous carcinoma cell growth and invasion (22 views)
J Exp Clin Cancer Res (ISSN: 0392-9078linking), 2022 Apr 2; 41(1): 122-122.
Impact Factor: 12.658
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Di Fiore A, Supuran CT, Scaloni A, De Simone G
* Post-translational modifications in tumor-associated carbonic anhydrases (22 views)
Amino Acids (ISSN: 0939-4451linking, 1438-2199electronic), 2022 Apr; 54(4): 543-558.
Impact Factor: 3.46
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Akgül Ö, Lucarini E, Mannelli LDC, Ghelardini C, D'Xambrosio K, Buonanno M, Monti SM, De Simone G, Angeli A, Supuran CT, Carta F
* Sultam based Carbonic Anhydrase VII inhibitors for the management of neuropathic pain (17 views)
Eur J Med Chem (ISSN: 0223-5234linking), 2022 Jan 5; 227: 113956-113956.
Impact Factor: 7.088
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Pagnozzi D, Pala N, Biosa G, Dallocchio R, Dessì A, Singh PK, Rogolino D, Di Fiore A, De Simone G, Supuran CT, Sechi M
* Interaction Studies between Carbonic Anhydrase and a Sulfonamide Inhibitor by Experimental and Theoretical Approaches (7 views)
Acs Med Chem Lett, 2022; 13: 271-277.
Impact Factor: 4.632
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Urbański LJ, Angeli A, Hytönen VP, Di Fiore A, De Simone G, Parkkila S, Supuran CT
* Inhibition of the β-carbonic anhydrase from the protozoan pathogen Trichomonas vaginalis with sulphonamides (148 views)
J Enzym Inhib Med Ch (ISSN: 1475-6366linking, 1475-6374electronic), 2021 Dec; 36(1): 329-334.
Impact Factor: 4.673
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Mancuso F, Di Fiore A, De Luca L, Angeli A, De Simone G, Supuran CT, Gitto R
* Design, synthesis and biochemical evaluation of novel carbonic anhydrase inhibitors triggered by structural knowledge on hCA VII (27 views)
Bioorg Med Chem (ISSN: 0968-0896linking, 1464-3391), 2021 Aug 15; 44: 116279-116279.
Impact Factor: 3.641
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Alterio V, Langella E, Buonanno M, Esposito D, Nocentini A, Berrino E, Bua S, Polentarutti M, Supuran CT, Monti SM, De Simone G
* Zeta-carbonic anhydrases show CS(2) hydrolase activity: A new metabolic carbon acquisition pathway in diatoms? (26 views)
Comput Struct Biotechnol J (ISSN: 2001-0370linking), 2021 Jun 5; 19: 3427-3436.
Impact Factor: 7.271
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Mulliri S, Laaksonen A, Spanu P, Farris R, Farci M, Mingoia F, Roviello GN, Mocci F
* Spectroscopic and In Silico Studies on the Interaction of Substituted Pyrazolo[1, 2-a]benzo[1, 2, 3, 4]tetrazine-3-one Derivatives with c-Myc G4-DNA (25 views)
Int J Mol Sc (ISSN: 1422-0067linking, 1422-0067electronic, 1661-6596), 2021 Jun 2; 22(11): 6028-6028.
Impact Factor: 5.923
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De Simone G, Bua S, Supuran CT, Alterio V
* Benzyl alcohol inhibits carbonic anhydrases by anchoring to the zinc coordinated water molecule (11 views)
Biochem Biophys Res Commun (ISSN: 0006-291xlinking), 2021 Apr 9; 548: 217-221.
Impact Factor: 3.575
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Langella E, Buonanno M, De Simone G, Monti SM
* Intrinsically disordered features of carbonic anhydrase IX proteoglycan-like domain (30 views)
Cell Mol Life Sci (ISSN: 1420-682xlinking), 2021 Mar; 78(5): 2059-2067.
Impact Factor: 9.261
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D’ambrosio K, Di Fiore A, Buonanno M, Kumari S, Tiwari M, Supuran CT, Mishra CB, Monti SM, De Simone G
* The crystal structures of 2-(4-benzhydrylpiperazin-1-yl)-N-(4-sulfamoylphenyl)acetamide in complex with human carbonic anhydrase II and VII provide insights into selective CA inhibitor development (84 views)
New Journal Of Chemistry, 2021; 45: 147-152.
Impact Factor: 3.288
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Urbański LJ, Di Fiore A, Azizi L, Hytönen VP, Kuuslahti M, Buonanno M, Monti SM, Angeli A, Zolfaghari Emameh R, Supuran CT, De Simone G, Parkkila S
* Biochemical and structural characterisation of a protozoan beta-carbonic anhydrase from Trichomonas vaginalis (125 views)
J Enzym Inhib Med Ch (ISSN: 1475-6366linking, 1475-6374electronic), 2020 Dec; 35(1): 1292-1299.
Impact Factor: 4.673
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Di Fiore A, Supuran CT, Scaloni A, De Simone G
* Human carbonic anhydrases and post-translational modifications: a hidden world possibly affecting protein properties and functions (122 views)
J Enzym Inhib Med Ch (ISSN: 1475-6366linking, 1475-6374electronic), 2020 Dec; 35(1): 1450-1461.
Impact Factor: 4.673
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Urbański LJ, Angeli A, Hytönen VP, Di Fiore A, Parkkila S, De Simone G, Supuran CT
* Inhibition of the newly discovered β‑carbonic anhydrase from the protozoan pathogen Trichomonas vaginalis with inorganic anions and small molecules (79 views)
J Chem Res (ISSN: 0162-0134linking, 0162-0134print), 2020 Dec; 213: 111274-111274.
Impact Factor: 3.212
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Sarnella A, D'Avino G, Hill BS, Alterio V, Winum JY, Supuran CT, De Simone G, Zannetti A
* A Novel Inhibitor of Carbonic Anhydrases Prevents Hypoxia-Induced TNBC Cell Plasticity (67 views) (PDF 25 views)
Int J Mol Sc (ISSN: 1422-0067linking, 1422-0067electronic, 1661-6596), 2020 Nov 9; 21(21): N/D-N/D.
Impact Factor: 4.556
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D'Ambrosio K, Carradori S, Cesa S, Angeli A, Monti SM, Supuran CT, De Simone G
* Catechols: a new class of carbonic anhydrase inhibitors (85 views)
Chem Commun (ISSN: 1359-7345linking, 1364-548xelectronic), 2020 Nov 4; 56(85): 13033-13033.
Impact Factor: 5.996
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Angeli A, Carta F, Nocentini A, Winum J, Zalubovskis R, Akdemir A, Onnis V, Eldehna WM, Capasso C, De Simone G, Monti Simona M, Carradori S, Donald WA, Dedhar S, Supuran CT
* Carbonic Anhydrase Inhibitors Targeting Metabolism and Tumor Microenvironment (83 views)
Metabolites, 2020 Oct 14; 10: 412-412.
Impact Factor: 4.097
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Bozdag M, Supuran CT, Esposito D, Angeli A, Carta F, Monti SM, De Simone G, Alterio V
* 2-Mercaptobenzoxazoles: a class of carbonic anhydrase inhibitors with a novel binding mode to the enzyme active site (101 views)
Chem Commun (ISSN: 1359-7345linking, 1364-548xelectronic), 2020 Jul 23; 56(59): 8297-8300.
Impact Factor: 5.996
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Nocentini A, Alterio V, Bua S, Micheli L, Esposito D, Buonanno M, Bartolucci G, Osman SM, Alothman ZA, Cirilli R, Pierini M, Monti SM, Di Cesare Mannelli L, Gratteri P, Ghelardini C, De Simone G, Supuran CT
* Phenyl(thio)phosphon(amid)ate Benzenesulfonamides as Potent and Selective Inhibitors of Human Carbonic Anhydrases II and VII Counteract Allodynia in a Mouse Model of Oxaliplatin-Induced Neuropathy (111 views)
J Med Chem (ISSN: 0022-2623linking, 0022-2623print), 2020 May 28; 63(10): 5185-5200.
Impact Factor: 6.205
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Mancuso F, Di Fiore A, De Luca L, Angeli A, Monti SM, De Simone G, Supuran CT, Gitto R
* Looking toward the Rim of the Active Site Cavity of Druggable Human Carbonic Anhydrase Isoforms (109 views)
Acs Med Chem Lett (ISSN: 1948-5875linking), 2020 May 14; 11(5): 1000-1005.
Impact Factor: 3.975
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Fik-jaskółka MA, Mkrtchyan AF, Saghyan AS, Palumbo R, Belter A, Hayriyan LA, Simonyan H, Roviello V, Roviello GN
* Spectroscopic and SEM evidences for G4-DNA binding by a synthetic alkyne-containing amino acid with anticancer activity (209 views) (PDF 75 views)
Spectrochim Acta A (ISSN: 1386-1425linking), 2020 Mar 15; 229: 117884-117884.
Impact Factor: 3.232
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Langella E, Buonanno M, De Simone G, Monti SM
* Intrinsically disordered features of carbonic anhydrase IX proteoglycan-like domain (94 views)
Cell Mol Life Sci (ISSN: 1420-682xlinking), 2020; 21: 8405-8405.
Impact Factor: 6.496
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Alterio V, Kellner M, Esposito D, Liesche-starnecker F, Bua S, Supuran CT, Monti SM, Zeidler R, De Simone G
* Biochemical and structural insights into Carbonic Anhydrase XII/Fab6A10 complex (168 views)
J Mol Biol (ISSN: 0022-2836linking, 1089-8638), 2019 Dec 6; 431(24): 4910-4921.
Impact Factor: 5.067
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De Simone G, Di Fiore A, Truppo E, Langella E, Vullo D, Supuran CT, Monti SM
* Exploration of the residues modulating the catalytic features of human carbonic anhydrase XIII by a site-specific mutagenesis approach (222 views)
J Enzym Inhib Med Ch (ISSN: 1475-6366linking, 1475-6374electronic), 2019 Dec; 34(1): 1506-1510.
Impact Factor: 4.027
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Langella E, Alterio V, D'Ambrosio K, Cadoni R, Winum JY, Supuran CT, Monti SM, De Simone G, Di Fiore A
* Exploring benzoxaborole derivatives as carbonic anhydrase inhibitors: a structural and computational analysis reveals their conformational variability as a tool to increase enzyme selectivity (243 views)
J Enzym Inhib Med Ch (ISSN: 1475-6366linking, 1475-6374electronic), 2019 Dec; 34(1): 1498-1505.
Impact Factor: 4.027
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Buemi MR, Di Fiore A, De Luca L, Angeli A, Mancuso F, Ferro S, Monti SM, Buonanno M, Russo E, De Sarro G, De Simone G, Supuran CT, Gitto R
* Exploring structural properties of potent human carbonic anhydrase inhibitors bearing a 4-(cycloalkylamino-1-carbonyl)benzenesulfonamide moiety (323 views)
Eur J Med Chem (ISSN: 1768-3254electronic, 0223-5234linking), 2019 Feb 1; 163: 443-452.
Impact Factor: 4.833
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De Simone G
* Targeted treatment of anaerobic cancer. Patent evaluation of US2016279084 and US2017056350 (225 views)
Expert Opin Ther Pat (ISSN: 1744-7674electronic, 1354-3776linking), 2019 Jan; 29(1): 1-6.
Impact Factor: 3.699
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Alterio V, Esposito D, Monti SM, Supuran CT, De Simone G
* Crystal structure of the human carbonic anhydrase II adduct with 1-(4-sulfamoylphenyl-ethyl)-2, 4, 6-triphenylpyridinium perchlorate, a membrane-impermeant, isoform selective inhibitor (533 views)
J Enzym Inhib Med Ch (ISSN: 1475-6374electronic, 1475-6366linking), 2018 Dec; 33(1): 151-157.
Impact Factor: 4.293
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Monti SM, Meccariello A, Ceruso M, Szafranski K, Slawinski J, Supuran CT
* Inhibition studies of Brucella suis beta-carbonic anhydrases with a series of 4-substituted pyridine-3-sulphonamides (369 views)
J Enzym Inhib Med Ch (ISSN: 1475-6374electronic, 1475-6366linking), 2018 Dec; 33(1): 255-259.
Impact Factor: 2.332
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Angeli A, Buonanno M, Donald WA, Monti SM, Supuran CT
* The zinc - but not cadmium - containing zeta-carbonic from the diatom Thalassiosira weissflogii is potently activated by amines and amino acids (279 views)
Bioorg Chem (ISSN: 1090-2120electronic, 0045-2068linking), 2018 Oct; 80: 261-265.
Impact Factor: 3.929
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De Simone G, Angeli A, Bozdag M, Supuran CT, Winum JY, Monti SM, Alterio V
* Inhibition of carbonic anhydrases by a substrate analog: benzyl carbamate directly coordinates the catalytic zinc ion mimicking bicarbonate binding (243 views)
Chem Commun (ISSN: 1364-548xelectronic, 1359-7345linking), 2018 Sep 11; 54(73): 10312-10315.
Impact Factor: 6.169
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Langella E, Buonanno M, Vullo D, Dathan N, Leone M, Supuran C, De Simone G, Monti SM
* Biochemical, biophysical and molecular dynamics studies on the proteoglycan-like domain of carbonic anhydrase IX (317 views)
Cell Mol Life Sci (ISSN: 1420-682xlinking), 2018 Sep; 75(17): 3283-3296.
Impact Factor: 6.721
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Supuran CT, Alterio V, Di Fiore A, D'Ambrosio K, Carta F, Monti SM, De Simone G
* Inhibition of carbonic anhydrase IX targets primary tumors, metastases, and cancer stem cells: Three for the price of one (532 views)
Med Res Rev (ISSN: 1098-1128electronic, 0198-6325linking), 2018 Sep; 38(6): 1799-1836.
Impact Factor: 8.29
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Mishra CB, Kumari S, Angeli A, Bua S, Buonanno M, Monti SM, Tiwari M, Supuran CT
* Discovery of potent anti-convulsant carbonic anhydrase inhibitors: Design, synthesis, in vitro and in vivo appraisal (234 views)
Eur J Med Chem (ISSN: 0223-5234linking, 1768-3254electronic), 2018 Aug 5; 156: 430-443.
Impact Factor: 4.816
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Di Fiore A, Monti DM, Scaloni A, De Simone G, Monti SM
* Protective Role of Carbonic Anhydrases III and VII in Cellular Defense Mechanisms upon Redox Unbalance (214 views)
Oxid Med Cell Longev (ISSN: 1942-0994linking), 2018 Aug 5; 2018:2018306: 2018306-2018306.
Impact Factor: 4.936
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Buonanno M, Di Fiore A, Langella E, D’ambrosio K, Supuran CT, Monti SM, De Simone G
* The Crystal Structure of a hCA VII Variant Provides Insights into the Molecular Determinants Responsible for Its Catalytic Behavior (303 views)
Int J Mol Sc (ISSN: 1661-6596, 1422-0067, 1422-0067electronic), 2018 May; 19(6): 19-24.
Impact Factor: 3.687
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D'Ambrosio K, Supuran CT, De Simone G
* Are Carbonic Anhydrases Suitable Targets to Fight Protozoan Parasitic Diseases? (250 views)
Curr Med Chem (ISSN: 1875-533xelectronic, 0929-8673linking), 2018; 25(39): 5266-5278.
Impact Factor: 4.63
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De Simone G, Langella E, Esposito D, Supuran CT, Monti SM, Winum JY, Alterio V
* Insights into the binding mode of sulphamates and sulphamides to hCA II: crystallographic studies and binding free energy calculations (251 views)
J Enzym Inhib Med Ch (ISSN: 1475-6366, 1475-6374electronic, 1475-6366linking), 2017 Dec; 32(1): 1002-1011.
Impact Factor: 3.638
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Monti DM, De Simone G, Langella E, Supuran CT, Di Fiore A, Monti SM
* Insights into the role of reactive sulfhydryl groups of Carbonic Anhydrase III and VII during oxidative damage (354 views)
J Enzym Inhib Med Ch (ISSN: 1475-6366, 1475-6374electronic, 1475-6366linking), 2017 Dec; 32(1): 5-12.
Impact Factor: 3.638
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Marchiori MF, Riul TB, Oliveira Bortot L, Andrade P, Junqueira GG, Foca G, Doti N, Ruvo M, Dias-baruffi M, Carvalho I, Campo VL
* Binding of triazole-linked galactosyl arylsulfonamides to galectin-3 affects Trypanosoma cruzi cell invasion (1018 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 0968-0896linking), 2017 Nov 1; 25(21): 6049-6059.
Impact Factor: 2.881
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Brunò E, Buemi MR, Di Fiore A, De LucaL, Ferro S, Angeli A, Cirilli R, Sadutto D, Alterio V, Monti SM, Supuran CT, De Simone G, Gitto R
* Probing Molecular Interactions between Human Carbonic Anhydrases (hCAs) and a Novel Class of Benzenesulfonamides (385 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2017 May 25; 60(10): 4316-4326.
Impact Factor: 6.253
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Buonanno M, Langella E, Zambrano N, Succoio M, Sasso E, Alterio V, Di Fiore A, Sandomenico A, Supuran CT, Scaloni A, Monti SM, De Simone G
* Disclosing the Interaction of Carbonic Anhydrase IX with Cullin-Associated NEDD8-Dissociated Protein 1 by Molecular Modeling and Integrated Binding Measurements (279 views)
Acs Chem Biol (ISSN: 1554-8929), 2017 Apr 19; N/D: N/D-N/D.
Impact Factor: 4.592
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Mishra CB, Kumari S, Angeli A, Monti SM, Buonanno M, Tiwari M, Supuran CT
* Discovery of Benzenesulfonamides with Potent Human Carbonic Anhydrase Inhibitory and Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Assessment (829 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2017 Mar 23; 60(6): 2456-2469.
Impact Factor: 6.253
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Altug C, Gunes H, Nocentini A, Monti SM, Buonanno M, Supuran CT
* Synthesis of isoxazole-containing sulfonamides with potent carbonic anhydrase II and VII inhibitory properties (301 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 0968-0896linking), 2017 Feb 15; 25(4): 1456-1464.
Impact Factor: 2.881
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Angapelly S, Ramya PV, Angeli A, Monti SM, Buonanno M, Alvala M, Supuran CT, Arifuddin M
* Discovery of 4-sulfamoyl-phenyl-beta-lactams as a new class of potent carbonic anhydrase isoforms I, II, IV and VII inhibitors: The first example of subnanomolar CA IV inhibitors (304 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 0968-0896linking), 2017 Jan 15; pii:S0968-0896(16): 539-544.
Impact Factor: 2.881
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Martínez-fernández L, Granucci G, Pollum M, Crespo-hernández CE, Persico M, Corral I
* Decoding the Molecular Basis for the Population Mechanism of the Triplet Phototoxic Precursors in UVA Light-Activated Pyrimidine Anticancer Drugs (363 views)
Chemistry (ISSN: 0947-6539, 1521-3765, 1521-3765electronic), 2017; 23(11): 2619-2627.
Impact Factor: 5.16
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Angapelly S, Ramya PVS, Angeli A, Monti SM, Buonanno M, Alvala M, Supuran CT, Arifuddin M
* Discovery of 4-sulfamoyl-phenyl-β-lactams as a new class of potent carbonic anhydrase isoforms I, II, IV and VII inhibitors: The first example of subnanomolar CA IV inhibitors (255 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 0968-0896linking), 2017; 25(2): 539-544.
Impact Factor: 2.881
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Alterio V, Cadoni R, Esposito D, Vullo D, Fiore AD, Monti SM, Caporale A, Ruvo M, Sechi M, Dumy P, Supuran CT, De Simone G, Winum JY
* Benzoxaborole as a new chemotype for carbonic anhydrase inhibition (434 views)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2016 Sep 29; 52(80): 11983-11986.
Impact Factor: 6.319
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Vullo D, Supuran CT, Scozzafava A, De Simone G, Monti SM, Alterio V, Carta F
* Kinetic and X-ray crystallographic investigations of substituted 2-thio-6-oxo-1, 6-dihydropyrimidine-benzenesulfonamides acting as carbonic anhydrase inhibitors (254 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 0968-0896linking), 2016 Aug 15; 24(16): 3643-3648.
Impact Factor: 2.93
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Di Fiore A, De Simone G, Alterio V, Riccio V, Winum JY, Carta F, Supuran CT
* The anticonvulsant sulfamide JNJ-26990990 and its S, S-dioxide analog strongly inhibit carbonic anhydrases: solution and X-ray crystallographic studies (249 views)
Org Biomol Chem (ISSN: 1477-0520, 1477-0539, 1477-0539electronic), 2016 Jun 07; 14(21): 4853-4858.
Impact Factor: 3.564
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Del Prete S, De Luca V, De Simone G, Supuran CT, Capasso C
* Cloning, expression and purification of the complete domain of the eta-carbonic anhydrase from Plasmodium falciparum (352 views)
J Enzym Inhib Med Ch (ISSN: 1475-6366, 1475-6374electronic, 1475-6366linking), 2016 Jun; 31(sup4): 54-59.
Impact Factor: 4.293
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Langella E, D'Ambrosio K, D'Ascenzio M, Carradori S, Monti SM, Supuran CT, De Simone G
* A Combined Crystallographic and Theoretical Study Explains the Capability of Carboxylic Acids to Adopt Multiple Binding Modes in the Active Site of Carbonic Anhydrases (335 views)
Chemistry (ISSN: 0947-6539, 1521-3765, 1521-3765electronic), 2016 Jan 4; 22(1): 97-100.
Impact Factor: 5.317
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Mishra CB, Kumari S, Angeli A, Monti SM, Buonanno M, Prakash A, Tiwari M, Supuran CT
* Design, synthesis and biological evaluation of N-(5-methyl-isoxazol-3-yl/1, 3, 4-thiadiazol-2-yl)-4-(3-substitutedphenylureido) benzenesulfonamides as human carbonic anhydrase isoenzymes I, II, VII and XII inhibitors (292 views)
J Enzyme Inhib Med Chem, 2016; 17: 1-6.
Impact Factor: 3.428
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Mollica A, Locatelli M, Macedonio G, Carradori S, Sobolev AP, De Salvador RF, Monti SM, Buonanno M, Zengin G, Angeli A, Supuran CT
* Microwave-assisted extraction, HPLC analysis, and inhibitory effects on carbonic anhydrase I, II, VA, and VII isoforms of 14 blueberry Italian cultivars (242 views)
J Enzyme Inhib Med Chem, 2016; 31(sup4): N/D-N/D.
Impact Factor: 3.428
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La Regina G, Coluccia A, Famiglini V, Pelliccia S, Monti L, Vullo D, Nuti E, Alterio V, De Simone G, Monti SM, Pan P, Parkkila S, Supuran CT, Rossello A, Silvestri R
* Discovery of 1, 1'-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors (335 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2015 Nov 12; 58(21): 8564-8572.
Impact Factor: 5.589
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Di Fiore A, Vergara A, Caterino M, Alterio V, Monti SM, Ombouma J, Dumy P, Vullo D, Supuran CT, Winum JY, De Simone G
* Hydroxylamine-O-sulfonamide is a versatile lead compound for the development of carbonic anhydrase inhibitors (320 views) (PDF 223 views)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2015 Jul 2; 51(57): 11519-11522.
Impact Factor: 6.567
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De Simone G, Monti SM, Alterio V, Buonanno M, De Luca V, Rossi M, Carginale V, Supuran CT, Capasso C, Di Fiore A
* Crystal structure of the most catalytically effective carbonic anhydrase enzyme known, SazCA from the thermophilic bacterium Sulfurihydrogenibium azorense (304 views)
Bioorg Med Chem Lett (ISSN: 0960-894x), 2015 May 1; 25(9): 2002-2006.
Impact Factor: 2.486
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Alterio V, Tanc M, Ivanova J, Zalubovskis R, Vozny I, Monti SM, Di Fiore A, De Simone G, Supuran CT
* X-ray crystallographic and kinetic investigations of 6-sulfamoyl-saccharin as a carbonic anhydrase inhibitor (344 views)
Org Biomol Chem (ISSN: 1477-0520, 1477-0539, 1477-0539electronic), 2015 Apr 7; 13(13): 4064-4069.
Impact Factor: 3.559
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De Simone G, Di Fiore A, Capasso C, Supuran CT
* The zinc coordination pattern in the eta-carbonic anhydrase from Plasmodium falciparum is different from all other carbonic anhydrase genetic families (471 views)
Bioorg Med Chem Lett (ISSN: 0960-894x), 2015 Apr 1; 25(7): 1385-1389.
Impact Factor: 2.486
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Alterio V, Langella E, De Simone G, Monti SM
* Cadmium-containing carbonic anhydrase CDCA1 in marine diatom Thalassiosira weissflogii (630 views)
Mar Drugs (ISSN: 1660-3397, 1660-3397linking), 2015 Mar 25; 13(4): 1688-1697.
Impact Factor: 3.345
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Monti SM, Supuran CT, De Simone G
* DPP-4 inhibitors: a patent review (2012 - 2014) (573 views)
Expert Opin Ther Pat (ISSN: 1354-3776, 1744-7674electronic), 2015 Feb; 25(2): 209-236.
Impact Factor: 4.626
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Supuran CT, Capasso C, De Simone G
* Carbonic Anhydrase II as Target for Drug Design (262 views)
Carbonic Anhydrases As Biocatalysts, 2015 Jan 08; N/D: 51-90.
Impact Factor: 0
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Monti SM, Supuran CT, De Simone G, Di Fiore A
* Carbonic Anhydrase VII (215 views)
Carbonic Anhydrases As Biocatalysts, 2015 Jan 08; N/D: 151-168.
Impact Factor: 0
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Supuran CT, De Simone G
Carbonic Anhydrases: An Overview (234 views)
Carbonic Anhydrases As Biocatalysts, 2015 Jan 08; N/D: 3-13.
Impact Factor: 0
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D'Ambrosio K, De Simone G, Supuran CT
* Human Carbonic Anhydrases: Catalytic Properties, Structural Features, and Tissue Distribution (281 views)
Carbonic Anhydrases As Biocatalysts, 2015 Jan 08; N/D: 17-30.
Impact Factor: 0
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D'Ambrosio K, Carradori S, Monti SM, Buonanno M, Secci D, Vullo D, Supuran CT, De Simone G
* Out of the active site binding pocket for carbonic anhydrase inhibitors (406 views) (PDF 237 views)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2015 Jan 7; 51(2): 302-305.
Impact Factor: 6.567
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Ceruso M, Carta F, Osman SM, Alothman Z, Monti SM, Supuran CT
* Inhibition studies of bacterial, fungal and protozoan β-class carbonic anhydrases with Schiff bases incorporating sulfonamide moieties (367 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 0968-0896linking), 2015; 23(15): 4181-4187.
Impact Factor: 2.923
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Iqbal J, Al-rashida M, Durdagi S, Alterio V, Di Fiore A
* Recent developments of carbonic anhydrase inhibitors as potential drugs (423 views)
Biomed Res Int (ISSN: 2314-6133, 2314-6141), 2015; 2015: 174178-174178.
Impact Factor: 2.134
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Di Fiore A, Alterio V, Monti SM, De Simone G, D’Ambrosio K
* Thermostable carbonic anhydrases in biotechnological applications (487 views)
Int J Mol Sc (ISSN: 1422-0067, 1661-6596, 1422-0067linking), 2015; 16(7): 15456-15480.
Impact Factor: 3.257
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Dathan NA, Alterio V, Troiano E, Vullo D, Ludwig M, De Simone G, Supuran CT, Monti SM
* Biochemical Characterization Of The Chloroplastic β-Carbonic Anhydrase From Flaveria Bidentis (l. ) "kuntze" (449 views)
J Enzym Inhib Med Ch (ISSN: 1475-6366, 1475-6374electronic, 1475-6366linking), 2014; 29(4): 500-504.
Impact Factor: 2.332
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De Simone G, Pizika G, Monti SM, Di Fiore A, Ivanova J, Vozny I, Trapencieris P, Zalubovskis R, Supuran CT, Alterio V
* Hydrophobic substituents of the phenylmethylsulfamide moiety can be used for the development of new selective carbonic anhydrase inhibitors (341 views)
Biomed Res Int (ISSN: 2314-6133, 2314-6141), 2014; 2014: 523210-523210.
Impact Factor: 1.579
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Alterio V, Pan P, Parkkila S, Buonanno M, Supuran CT, Monti SM, De Simone G
* The Structural Comparison Between Membrane-Associated Human Carbonic Anhydrases Provides Insights Into Drug Design Of Selective Inhibitors (416 views)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 2014; 101(7): 769-778.
Impact Factor: 2.385
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Alterio V, Monti SM, De Simone G
* Thermal-stable carbonic anhydrases: a structural overview (389 views)
Subcell Biochem (ISSN: 0306-0225), 2014; 75: 387-404.
Impact Factor: 33.116
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Rami M, Dubois L, Parvathaneni NK, Alterio V, van Kuijk SJ, Monti SM, Lambin P, De Simone G, Supuran CT, Winum JY
* Hypoxia-targeting carbonic anhydrase IX inhibitors by a new series of nitroimidazole-sulfonamides/sulfamides/sulfamates (546 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2013 Nov 14; 56(21): 8512-8520.
Impact Factor: 5.48
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De Simone G, Alterio V, Supuran CT
* Exploiting the hydrophobic and hydrophilic binding sites for designing carbonic anhydrase inhibitors (507 views)
Expert Opin Drug Discov (ISSN: 1746-0441), 2013 Jul; 8(7): 793-810.
Impact Factor: 3.467
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Di Fiore A, Capasso C, De Luca V, Monti SM, Carginale V, Supuran CT, Scozzafava A, Pedone C, Rossi M, De Simone G
* X-ray structure of the first 'extremo-alpha-carbonic anhydrase', a dimeric enzyme from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 (515 views)
Acta Crystallogr D Biol Crystallogr (ISSN: 0907-4449, 0907-4449linking), 2013 Jun; 69(6): 1150-1159.
Impact Factor: 7.232
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Monti SM, De Simone G, Dathan NA, Ludwig M, Vullo D, Scozzafava A, Capasso C, Supuran CT
* Kinetic And Anion Inhibition Studies Of A Beta-Carbonic Anhydrase (fbica 1) From The C-4 Plant Flaveria Bidentis (440 views)
Bioorg Med Chem Lett (ISSN: 0960-894x), 2013 Mar 15; 23(6): 1626-1630.
Impact Factor: 2.331
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Buanne P, Renzone G, Monteleone F, Vitale M, Monti SM, Sandomenico A, Garbi C, Montanaro D, Accardo M, Troncone G, Zatovicova M, Csaderova L, Supuran CT, Pastorekova S, Scaloni A, De Simone G, Zambrano N
* Characterization of carbonic anhydrase ix interactome reveals proteins assisting its nuclear localization in hypoxic cells (393 views)
J Proteome Res (ISSN: 1535-3893), 2013 Jan; 12(1): 282-292.
Impact Factor: 5.001
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Del Giudice R, Monti DM, Truppo E, Arciello A, Supuran CT, De Simone G, Monti SM
* Human Carbonic Anhydrase Vii Protects Cells From Oxidative Damage (366 views)
Biol Chem Biological Chemistry (ISSN: 1431-6730, 1431-1673, 1437-4315), 2013; 394(10): 1343-1348.
Impact Factor: 2.689
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Alterio V, Di Fiore A, D'Ambrosio K, Supuran CT, De Simone G
* Multiple binding modes of inhibitors to carbonic anhydrases: How to design specific drugs targeting 15 different isoforms? (452 views)
Chem Rev (ISSN: 0009-2665), 2012 Sep; 112(8): 4421-4468.
Impact Factor: 41.298
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De Simone G, Supuran CT
* (In)organic anions as carbonic anhydrase inhibitors (379 views)
J Chem Res (ISSN: 0162-0134, 1873-3344, 0162-0134print), 2012 Jun; 111: 117-129.
Impact Factor: 3.197
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Alterio V, Langella E, Viparelli F, Vullo D, Ascione G, Dathan NA, Morel FM, Supuran CT, De Simone G, Monti SM
* Structural and inhibition insights into carbonic anhydrase CDCA1 from the marine diatom Thalassiosira weissflogii (435 views)
Biochimie (ISSN: 0300-9084, 1638-6183, 1638-6183electronic), 2012 May; 94(5): 1232-1241.
Impact Factor: 3.142
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Zannetti A, Iommelli F, Speranza A, Salvatore M, Del Vecchio S
* 3'-deoxy-3'-18F-fluorothymidine (FLT) PET/CT to guide therapy with epidermal growth factor receptor (EGFR) antagonists and Bcl-xL inhibitors in non-small cell lung cancer (614 views)
J Nucl Med (ISSN: 0161-5505, 1535-5667, 1535-5667electronic), 2012 Mar 1; 53(3): 443-450.
Impact Factor: 5.774
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Zannetti A, Iommelli F, Speranza A, Salvatore M, Del Vecchio S
* 3'-deoxy-3'-18F-fluorothymidine PET/CT to guide therapy with epidermal growth factor receptor antagonists and Bcl-xL inhibitors in non-small cell lung cancer (525 views)
J Nucl Med (ISSN: 1535-5667, 0161-5505, 1535-5667electronic), 2012 Mar 1; 53(3): 443-450.
Impact Factor: 5.774
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Truppo E, Supuran CT, Sandomenico A, Vullo D, Innocenti A, Di Fiore A, Alterio V, De Simone G, Monti SM
* Carbonic anhydrase VII is S-glutathionylated without loss of catalytic activity and affinity for sulfonamide inhibitors (384 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2012 Feb 15; 22(4): 1560-1564.
Impact Factor: 2.338
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Monti SM, Supuran CT, De Simone G
* Carbonic anhydrase IX as a target for designing novel anticancer drugs (526 views)
Curr Med Chem (ISSN: 0929-8673, 1875-533x, 1875-533xelectronic), 2012 Feb; 19(6): 821-830.
Impact Factor: 4.07
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De Simone G
* Editorial: Zinc Metallo-Enzymes As Target For Drug Design (423 views)
Curr Med Chem (ISSN: 0929-8673, 1875-533x, 1875-533xelectronic), 2012 Feb; 19(6): 820-1012.
Impact Factor: 4.07
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Monti SM, Maresca A, Viparelli F, Carta F, De Simone G, Muehlschlegel FA, Scozzafava A, Supuran CT
* Dithiocarbamates are strong inhibitors of the beta-class fungal carbonic anhydrases from Cryptococcus neoformans, Candida albicans and Candida glabrata (392 views)
Bioorg Med Chem Lett (ISSN: 0960-894x), 2012 Jan 15; 22(2): 859-862.
Impact Factor: 2.338
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D'Ambrosio K, Smaine F-Z, Carta F, De Simone G, Winum J-Y, Supuran CT
* Development of potent carbonic anhydrase inhibitors incorporating both sulfonamide and sulfamide groups (467 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2012; 55(15): 6776-6783.
Impact Factor: 5.614
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Sorriento D, Santulli G, Del Giudice C, Anastasio A, Trimarco B, Iaccarino G
* Endothelial cells are able to synthesize and release catecholamines both in vitro and in vivo (423 views)
Hypertensionhypertension (ISSN: 0194-911x), 2012; 60(1): 129-136.
Impact Factor: 6.873
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Di Fiore A, Maresca A, Supuran CT, De Simone G
* Hydroxamate represents a versatile zinc binding group for the development of new carbonic anhydrase inhibitors (361 views)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2012; 48(70): 8838-8840.
Impact Factor: 6.378
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Caraci F, Molinaro G, Battaglia G, Giuffrida ML, Riozzi B, Traficante A, Bruno V, Cannella M, Merlo S, Wang X, Heinz BA, Nisenbaum ES, Britton TC, Drago F, Sortino MA, Copani A, Nicoletti F
* Targeting group II Metabotropic Glutamate (mGlu) receptors for the treatment of psychosis associated with alzheimer's disease: Selective activation of mGlu2 receptors amplifies β-amyloid toxicity in cultured neurons, whereas dual activation of mGlu2 and mGlu3 receptors is neuroprotective (748 views)
Mol Pharmacol (ISSN: 0026-895x), 2011 Mar; 79(3): 618-626.
Impact Factor: 4.883
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Di Fiore A, Maresca A, Alterio V, Supuran CT, De Simone G
* Carbonic anhydrase inhibitors: X-ray crystallographic studies for the binding of N-substituted benzenesulfonamides to human isoform II (338 views)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2011; 47(42): 11636-11638.
Impact Factor: 6.169
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Viparelli F, Monti SM, De Simone G, Innocenti A, Scozzafava A, Xu Y, Morel FMM, Supuran CT
* Inhibition Of The R1 Fragment Of The Cadmium-Containing Zeta-Class Carbonic Anhydrase From The Diatom Thalassiosira Weissflogii With Anions (333 views)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2010 Sep 15; 20(16): 4745-4748.
Impact Factor: 2.661
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Alterio V, Monti SM, Truppo E, Pedone C, Supuran CT, De Simone G
* The first example of a significant active site conformational rearrangement in a carbonic anhydrase-inhibitor adduct: The carbonic anhydrase I-topiramate complex (446 views)
Org Biomol Chem (ISSN: 1477-0520, 1477-0539, 1477-0539electronic), 2010 Sep 7; 8(15): 3528-3533.
Impact Factor: 3.451
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Di Fiore A, Truppo E, Supuran CT, Alterio V, Dathan N, Bootorabi F, Parkkila S, Monti SM, De Simone G
* Crystal structure of the C183S/C217S mutant of human CA VII in complex with acetazolamide (325 views)
Bioorg Med Chem Lett (ISSN: 0960-894x), 2010 Sep 1; 20(17): 5023-5026.
Impact Factor: 2.661
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Di Fiore A, Monti SM, Innocenti A, Winum J-Y, De Simone G, Supuran CT
* Carbonic anhydrase inhibitors: Crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV (352 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2010 Jun 15; 20(12): 3601-3605.
Impact Factor: 2.661
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De Simone G, Supuran CT
* Carbonic anhydrase IX: Biochemical and crystallographic characterization of a novel antitumor target (398 views)
Bba-Gen Subjects (ISSN: 1570-9639, 0006-3002, 0925-4439), 2010 Feb; 1804(2): 404-409.
Impact Factor: 2.773
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Guler OO, De Simone G, Supuran CT
* Drug design studies of the novel antitumor targets carbonic anhydrase IX and XII (540 views)
Curr Med Chem (ISSN: 0929-8673, 1875-533x, 1875-533xelectronic), 2010; 17(15): 1516-1526.
Impact Factor: 4.63
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Supuran CT, Di Fiore A, Alterio V, Monti SM, De Simone G
* Recent advances in structural studies of the carbonic anhydrase family: The crystal structure of human CA IX and CA XIII (471 views)
Curr Pharm Des Current Pharmaceutical Design (ISSN: 1381-6128, 1873-4286), 2010; 16(29): 3246-3254.
Impact Factor: 4.774
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Innocenti A, Pastorekova S, Pastorek J, Scozzafava A, De Simone G, Supuran CT
* The proteoglycan region of the tumor-associated carbonic anhydrase isoform IX acts as anintrinsic buffer optimizing CO2 hydration at acidic pH values characteristic of solid tumors (264 views)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2009 Oct 15; 19(20): 5825-5828.
Impact Factor: 2.65
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Vitale RM, Alterio V, Innocenti A, Winum JY, Monti SM, De Simone G, Supuran CT
* Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis- sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors (462 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2009 Oct 8; 52(19): 5990-5998.
Impact Factor: 4.802
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Alterio V, Hilvo M, Di Fiore A, Supuran CT, Pan P, Parkkila S, Scaloni A, Pastorek J, Pastorekova S, Pedone C, Scozzafava A, Monti SM, De Simone G
* Crystal structure of the catalytic domain of the tumor-associated human carbonic anhydrase IX (571 views)
P Natl Acad Sci Usa (ISSN: 0027-8424, 1091-6490, 0027-8424print), 2009 Sep 22; 106(38): 16233-16238.
Impact Factor: 9.432
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De Simone G, Scozzafava A, Supuran CT
* Which Carbonic Anhydrases are Targeted by the Antiepileptic Sulfonamides and Sulfamates? (352 views)
Chem Biol Drug Des (ISSN: 1747-0277, 1747-0285), 2009 Sep; 74(3): 317-321.
Impact Factor: 2.473
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Di Fiore A, Monti SM, Hilvo M, Parkkila S, Romano V, Scaloni A, Pedone C, Scozzafava A, Supuran CT, De Simone G
* Crystal structure of human carbonic anhydrase XIII and its complex with the inhibitor acetazolamide (542 views)
Proteins (ISSN: 1097-0134, 0887-3585, 1097-0134electronic), 2009 Jan; 74(1): 164-175.
Impact Factor: 3.085
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Hilvo M, De Simone G, Supuran CT, Parkkila S
* Advances in the Inhibitory and Structural Investigations on Carbonic Anhydrase Isozymes XIII and XV (289 views)
Drug Des Of Zinc Enzyme Inhibitors (ISSN: 9780-4702, 9780-470275009), 2009; N/D: 273-283.
Impact Factor: 1.156
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De Simone G, Supuran CT
* Drug Design of Antiobesity Carbonic Anhydrase Inhibitors (332 views)
Drug Des Of Zinc Enzyme Inhibitors (ISSN: 9780-4702, 9780-470275009), 2009; 66(DECEMBERSPEC.I): 241-254.
Impact Factor: 1.156
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Alterio V, Di Fiore A, D'Ambrosio K, Supuran CT, De Simone G
* X-Ray Crystallography of Carbonic Anhydrase Inhibitors and Its Importance in Drug Design (426 views)
Drug Des Of Zinc Enzyme Inhibitors (ISSN: 9780-4702, 9780-470275009), 2009; N/D: 73-138.
Impact Factor: 1.156
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Hilvo M, Baranauskiene L, Salzano AM, Scaloni A, Matulis D, Innocenti A, Scozzafava A, Monti SM, Di Fiore A, De Simone G, Lindfors M, Janis J, Valjakka J, Pastorekova S, Pastorek J, Kulomaa MS, Nordlund HR, Supuran CT, Parkkila S
* Biochemical characterization of CA IX, one of the most active carbonic anhydrase isozymes (459 views)
Jbc Papers (ISSN: 0021-9258, 1083-351x, 0021-9258linking), 2008 Oct 10; 283(41): 27799-27809.
Impact Factor: 5.52
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D'Ambrosio K, Vitale R, Dogne J, Masereel B, Innocenti A, Scozzafava A, De Simone G, Supuran CT
* Ccarbonic Anhydrase Inhibitors: Bioreductive Nitro-Containing Sulfonamides With Selectivity For Targeting The Tumor Associated Isoforms Ix And Xii (823 views)
J Med Chem (ISSN: 1520-4804, 0022-2623, 0022-2623print), 2008 Jun 12; 51(11): 3230-3237.
Impact Factor: 4.898
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Supuran CT, Di Fiore A, De Simone G
* Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity (560 views)
Expert Opin Emerg Drugsexpert Opinion On Emerging Drugs (ISSN: 1472-8214), 2008 Jun; 13(2): 383-392.
Impact Factor: 3.08
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Di Fiore A, Pedone C, Antel J, Waldeck H, Witte A, Wurl M, Scozzafava A, Supuran CT, De Simone G
* Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors (385 views)
Bioorg Med Chem Lett (ISSN: 1464-3405, 0960-894x, 1464-3405electronic), 2008 Apr 15; 18(8): 2669-2674.
Impact Factor: 2.531
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Innocenti A, Scozzafava A, Parkkila S, Puccetti L, De Simone G, Supuran CT
* Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates (360 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2008 Apr 1; 18(7): 2267-2271.
Impact Factor: 2.531
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Leese MP, Jourdan FL, Gaukroger K, Mahon MF, Newman SP, Foster PA, Stengel C, Regis-Lydi S, Ferrandis E, Di Fiore A, De Simone G, Supuran CT, Purohit A, Reed MJ, Potter BVL
* Structure-activity relationships of C-17 cyano-substituted estratrienes as anticancer agents (462 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2008 Mar 13; 51(5): 1295-1308.
Impact Factor: 4.898
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De Simone G, Di Fiore A, Supuran CT
* Are carbonic anhydrase inhibitors suitable for obtaining antiobesity drugs? (472 views)
Curr Pharm Des Current Pharmaceutical Design (ISSN: 1381-6128, 1873-4286), 2008 Mar; 14(7): 655-660.
Impact Factor: 4.399
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D'Ambrosio K, Masereel B, Thiry A, Scozzafava A, Supuran CT, De Simone G
* Carbonic anhydrase inhibitors: Binding of indanesulfonamides to the human isoform II (378 views)
Chemmedchem (ISSN: 1860-7179, 1860-7187, 1860-7187electronic), 2008 Mar; 3(3): 473-477.
Impact Factor: 3.15
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Supuran CT, De Simone G
Carbonic anhydrases--an overview (354 views)
Curr Pharm Des, 2008; 14(7): 603-614.
Impact Factor: 0
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Hilvo M, Innocenti A, Monti SM, De Simone G, Supuran CT, Parkkila S
* Recent advances in research on the most novel carbonic anhydrases, CA XIII and XV (479 views)
Curr Pharm Des Current Pharmaceutical Design (ISSN: 1381-6128, 1873-4286), 2008; 14(7): 672-678.
Impact Factor: 4.399
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Alterio V, De Simone G, Monti SM, Scozzafava A, Supuran CT
* Carbonic anhydrase inhibitors: Inhibition of human, bacterial, and archaeal isozymes with benzene-1, 3-disulfonamides-Solution and crystallographic studies (329 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2007 Sep 1; 17(15): 4201-4207.
Impact Factor: 2.604
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Vitale RM, Pedone C, Amodeo P, Antel J, Wurl M, Scozzafava A, Supuran CT, De Simone G
* Molecular modeling study for the binding of zonisamide and topiramate to the human mitochondrial carbonic anhydrase isoform VA (335 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 1464-3391electronic), 2007 Jun 15; 15(12): 4152-4158.
Impact Factor: 2.662
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Di Fiore A, Scozzafava A, Winum JY, Montero JL, Pedone C, Supuran CT, De Simone G
* Carbonic anhydrase inhibitors: binding of an antiglaucoma glycosyl-sulfanilamide derivative to human isoform II and its consequences for the drug design of enzyme inhibitors incorporating sugar moieties (410 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2007 Mar 15; 17(6): 1726-1731.
Impact Factor: 2.604
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De Simone G, Supuran CT
* Antiobesity carbonic anhydrase inhibitors (474 views)
Curr Top Med Chem (ISSN: 1568-0266, 1568-0266linking, 1873-4294electronic), 2007; 7(9): 879-884.
Impact Factor: 4.325
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Leese MP, Leblond B, Smith A, Newman SP, Di Fiore A, De Simone G, Supuran CT, Purohit A, Reed MJ, Potter BVL
* 2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity (931 views)
J Med Chem (ISSN: 0022-2623print, 0022-2623linking, 1520-4804), 2006 Dec 28; 49(26): 7683-7696.
Impact Factor: 5.115
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Menchise V, De Simone G, Di Fiore A, Scozzafava A, Supuran CT
* Carbonic anhydrase inhibitors: X-ray crystallographic studies for the binding of 5-amino-1, 3, 4-thiadiazole-2-sulfonamide and 5-(4-amino-3-chloro-5-fluorophenylsulfonamido)1, 3, 4-thiadiazole-2-sulfon amide to human isoform II (310 views)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2006 Dec 15; 16(24): 6204-6208.
Impact Factor: 2.538
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De Simone G, Vitale RM, Di Fiore A, Pedone C, Scozzafava A, Montero JL, Winum JY, Supuran CT
* Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX (474 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2006 Sep 7; 49(18): 5544-5551.
Impact Factor: 5.115
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Alterio V, Vitale RM, Monti SM, Pedone C, Scozzafava A, Cecchi A, De Simone G, Supuran CT
* Carbonic anhydrase inhibitors: X-ray and molecular modeling study for the interaction of a fluorescent antitumor sulfonamide with isozyme II and IX (484 views)
J Am Chem Soc (ISSN: 0002-7863, 0002-2786, 1520-5126), 2006 Jun 28; 128(25): 8329-8335.
Impact Factor: 7.696
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Di Fiore A, Pedone C, D'Ambrosio K, Scozzafava A, De Simone G, Supuran CT
* Carbonic anhydrase inhibitors: Valdecoxib binds to a different active site region of the human isoform II as compared to the structurally related cyclooxygenase II 'selective' inhibitor celecoxib (323 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2006 Jan 15; 16(2): 437-442.
Impact Factor: 2.538
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Grasso G, D'Agata R, Rizzarelli E, Spoto G, D'Andrea LD, Pedone C, Picardi A, Romanelli A, Fragai M, Yeo KJ
* Activity of anchored human matrix metalloproteinase-1 catalytic domain on Au(111) surfaces monitored by ESI-MS (575 views)
J Mass Spectrom (ISSN: 1076-5174, 1096-9888), 2005 Dec; 40(12): 1565-1571.
Impact Factor: 3.574
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De Luca S, Della Moglie R, De Capua A, Morelli G
* New synthetic strategy for o-NBS protected amino acids and their use in synthesis of mono-benzylated peptides (447 views)
Tetrahedron Lett (ISSN: 0040-4039), 2005 Sep 26; 46(39): 6637-6640.
Impact Factor: 2.477
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Menchise V, De Simone G, Alterio V, Di Fiore A, Pedone C, Scozzafava A, Supuran CT
* Carbonic anhydrase inhibitors: Stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide complexed with isozyme II (482 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2005 Sep 8; 48(18): 5721-5727.
Impact Factor: 4.926
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De Simone G, Di Fiore A, Menchise V, Pedone C, Antel J, Casini A, Scozzafava A, Wurl M, Supuran CT
* Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studies (420 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2005 May 2; 15(9): 2315-2320.
Impact Factor: 2.478
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Di Fiore A, De Simone G, Menchise V, Pedone C, Casini A, Scozzafava A, Supuran CT
* Carbonic anhydrase inhibitors: X-ray crystal structure of a benzenesulfonamide strong CA II and CA IX inhibitor bearing a pentafluorophenylaminothioureido tail in complex with isozyme II (489 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2005 Apr 1; 15(7): 1937-1942.
Impact Factor: 2.478
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Fonti R, Latella G, Caprilli R, Frieri G, Marcheggiano A, Sambuy Y
Carbonic anhydrase I reduction in colonic mucosa of patients with active ulcerative colitis (432 views)
Digestive Diseases And Sciences (ISSN: 0163-2116), 1998; 43(9): 2086-2092.
Impact Factor: 1.972
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134 Records (133 excluding Abstracts).
Total impact factor: 615.627 (610.512 excluding Abstracts).
Total 5 year impact factor: 543.59 (538.086 excluding Abstracts).
Total impact factor: 615.627 (610.512 excluding Abstracts).
Total 5 year impact factor: 543.59 (538.086 excluding Abstracts).
468 views. Last view on Wednesday 15 March 2023, 16:17:34
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