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 (443 views visite)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2005 Sep 8; 48(18): 5721-5727.
Export to Esporta in BibTeX Export to Esporta in EndNote
Paper type Tipo di articolo: Journal Article,
Impact factor: 4.926, 5-year impact factor Impact factor a 5 anni: 5.504
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-24744467784&partnerID=40&md5=1c4ee242723e3de5189fb90a3acd55d9
Keywords Parole chiave: 1 N (4 Sulfamoylphenylethyl) 2, 6 Trimethylpyridinium Perchlorate, Carbonate Dehydratase Ii, Carbonate Dehydratase Inhibitor, Carbonate Dehydratase Xii, Glutamine, Isoenzyme, Leucine, Phenylalanine, Sulfonamide, Threonine, Unclassified Drug, Valine, Amino Acid Sequence, Antineoplastic Activity, Article, Complex Formation, Crystal Structure, Drug Binding Site, Drug Structure, Hydrophilicity, Hydrophobicity, Protein Expression, Protein Targeting, Structure Analysis, X Ray Crystallography, Antigens, Antineoplastic Agents, Carbonic Anhydrase Ii, Cell Membrane Permeability, X-Ray, Humans, Models, Molecular, Molecular Structure, Protein Binding, Pyridinium Compounds, Quantitative Structure-Activity Relationship, Recombinant Proteins, Tumor Markers, Biological,
Affiliations Affiliazioni:
*** IBB - CNR ***
Istituto di Biostrutture e Bioimmagini, CNR, via Mezzocannone 16, 80134 Naples, Italy
Bioindustry Park del Canavese Spa, Via Ribes 5, 10010 Colleretto Giacosa (Torino), Italy
Dipartimento delle Scienze Biologiche, Sezione Biostrutture, University of Naples Federico II, via Mezzocannone 16, 80134 Naples, Italy
Università degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence), Italy
Universit degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence), Italy
References Riferimenti:
Supuran, C.T., Scozzafava, A., Conway, J., (2004) Carbonic Anhydrase - Its Inhibitors and Activators, pp. 1-363. , CRC Press: Boca Rato
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
Pastorekova, S., Parkkila, S., Pastorek, J., Supuran, C.T., Carbonic anhydrases: Current state of the art, therapeutic applications and future prospects (2004) J. Enzyme. Inhib. Med. Chem., 19, pp. 199-229
Marquis, R.E., Whitson, J.T., Management of glaucoma: Focus on pharmacological therapy (2005) Drugs Aging, 22, pp. 1-21
Vullo, D., Innocenti, A., Nishimori, I., Pastorek, J., Scozzafava, A., Pastorekova, S., Supuran, C.T., Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides - A new target for the design of antitumor and antiglaucoma drugs? (2005) Bioorg. Med. Chem. Lett., 15, pp. 963-969
Supuran, C.T., Casini, A., Scozzafava, A., Development of sulfonamide carbonic anhydrase inhibitors (CAIs) (2004) Carbonic Anhydrase - Its Inhibitors and Activators, pp. 67-148. , Supuran, C. T., Scozzafava, A., Conway, J.
Eds., CRC Press: Boca Raton (FL), USA
Loiselle, F.B., Morgan, P.E., Alvarez, B.V., Casey, J.R., Regulation of the human NBC3 Na+/HCO3- Cotransporter by carbonic anhydrase II and PKA (2004) Am. J. Physiol. Cell Physiol., 286, pp. C1423-C1433
Rivera, C., Voipio, J., Kaila, K., Two developmental switches in GABAergic signalling: The K+-Cl- Cotransporter KCC2 and carbonic anhydrase CAVII (2005) J. Physiol., 562, pp. 27-36
Vullo, D., Voipio, J., Innocenti, A., Rivera, C., Ranki, H., Scozzafava, A., Kaila, K., Supuran, C.T., Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides (2005) Bioorg. Med. Chem. Lett., 15, pp. 971-976
Lyons, K.E., Pahwa, R., Cornelia, C.L., Eisa, M.S., Elble, R.J., Fahn, S., Jankovic, J., Watts, R.L., Benefits and risks of pharmacological treatments for essential tremor (2003) Drug Saf., 26, pp. 461-481
Garske, L.A., Brown, M.G., Morrison, S.C., Acetazolamide reduces exercise capacity and increases leg fatigue under hypoxic conditions (2003) J. Appl. Physiol., 94, pp. 991-996
Hori, K., Ishida, S., Inoue, M., Shinoda, K., Kawashima, S., Kitamura, S., Oguchi, Y., Treatment of cystoid macular edema with oral acetazolamide in a patient with best vitelliform macular dystrophy (2004) Retina, 24, pp. 481-482
Winum, J.Y., Scozzafava, A., Montera, J.L., Supuran, C.T., Sulfamates and their therapeutic potential (2005) Med. Res. Rev., 25, pp. 186-228
Svastova, E., Hulikova, A., Rafajova, M., Zat'ovicova, M., Gibadulinova, A., Casini, A., Cecchi, A., Pastorekova, S., Hypoxia activates the capacity of tumor-associated carbonic anhydrase IX to acidify extracellular pH (2004) FEBS Lett., 577, pp. 439-445
Pastorek, J., Pastorekova, S., Callebaut, I., Mornon, J.P., Zelnik, V., Opavsky, R., Zat'ovicova, M., Stanbridge, E.J., 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
Rafajova, M., Zatovicova, M., Kettmann, R., Pastorek, J., Pastorekova, S., Induction by hypoxia combined with low glucose or low bicarbonate and high posttranslational stability upon reoxygenation contribute to carbonic anhydrase IX expression in cancer cells (2004) Int. J. Oncol., 24, pp. 995-1004
Ivanov, S., Liao, S.Y., Ivanova, A., Danilkovitch-Miagkova, A., Tarasova, N., Weirich, G., Merrill, M.J., Stanbridge, E.J., Expression of hypoxia-inducible cell-surface transmembrane carbonic anhydrases in human cancer (2001) Am. J. Pathol., 158, pp. 905-919
Winum, J.Y., Pastorekova, S., Jakubickova, L., Montero, J.L., Scozzafava, A., Pastorek, J., Vullo, D., Supuran, C.T., Carbonic anhydrase inhibitors: Synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates (2005) Bioorg. Med. Chem. Lett., 15, pp. 579-584
Vullo, D., Franchi, M., Gallon, E., Pastorek, J., Scozzafava, A., Pastorekova, S., Supuran, C.T., Carbonic anhydrase inhibitors: Inhibition of the tumor-associated isozyme IX with aromatic and heterocyclic sulfonamides (2003) Bioorg. Med. Chem. Lett., 13, pp. 1005-1009
Krungkrai, J., Scozzafava, A., Reungprapavut, S., Krungkrai, S.R., Rattanajak, R., Kamchonwongpaisan, S., Supuran, C.T., Carbonic anhydrase inhibitors. Inhibition of Plasmodium falciparum carbonic anhydrase with aromatic sulfonamides: Towards antimalarials with a novel mechanism of action? (2005) Bioorg Med. Chem., 13, pp. 483-489
Covarrubias Suarez, A., Larsson, A.M., Ho Gbom, M., Lindberg, J., Bergfors, T., Bjo Rkelid, C., Mowbray, S.L., Jones, T.A., Structure and function of carbonic anhydrases from mycobacterium tuberculosis (2005) J. Biol. Chem., 280, pp. 18782-18789
Chakravarty, S., Kannan, K.K., Drug-protein interactions. Refined structures of three sulfonamide drug complexes of human carbonic anhydrase I enzyme (1994) J. Mol. Biol., 243, pp. 298-309
Vidgren, J., Svensson, A., Liljas, A., Refined structure of the aminobenzolamide complex of human carbonic anhydrase II at 1.9 A and sulphonamide modelling of bovine carbonic anhydrase III (1993) Int. J. Biol. Macromol., 15, pp. 97-100
Eriksson, A.E., Jones, T.A., Liljas, A., Refined structure of human carbonic anhydrase II at 2.0 Å resolution (1988) Proteins Struct. Funct., 4, pp. 274-282
Boriack, P.A., Christianson, D.W., Kingery-Wood, J., Whitesides, G.M., Secondary interactions significantly removed from the sulfonamide binding pocket of carbonic anhydrase II influence inhibitor binding constants (1995) J. Med. Chem., 38, pp. 2286-2291
Stams, T., Chen, Y., Boriack-Sjodin, P.A., Hurt, J.D., Liao, J., May, J.A., Dean, T., Christianson, D.W., Structures of murine carbonic anhydrase IV and human carbonic anhydrase II complexed with brinzolamide: Molecular basis of isozyme-drug discrimination (1998) Protein Sci., 7, pp. 556-563
Kim, C.Y., Chandra, P.P., Jain, A., Christianson, D.W., Fluoroaromatic-fluoroaromatic interactions between inhibitors bound in the crystal lattice of human carbonic anhydrase II (2001) J. Am. Chem. Soc., 123, pp. 9620-9627
Di Fiore, A., De Simone, G., Menchise, V., Pedone, C., Casini, A., Scozzafava, A., Supuran, C.T., 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 (2005) Bioorg. Med. Chem. Lett., 15, pp. 1937-1942
Abbate, F., Casini, A., Scozzafava, A., Supuran, C.T., Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the perfluorobenzoyl analogue of methazolamide. Implications for the drug design of fluorinated inhibitors (2003) J. Enzyme. Inhib. Med. Chem., 18, pp. 303-308
Casini, A., Abbate, F., Scozzafava, A., Supuran, C.T., Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with a bis-sulfonamide-two heads are better than one? (2003) Bioorg. Med. Chem. Lett., 13, pp. 2759-2763
Casini, A., Antel, J., Abbate, F., Scozzafava, A., David, S., Waldeck, H., Schafer, S., Supuran, C.T., Carbonic anhydrase inhibitors: SAR and X-ray crystallographic study for the interaction of sugar sulfamates/sulfamides with isozymes I, II and IV (2003) Bioorg. Med. Chem. Lett., 13, pp. 841-845
Abbate, F., Coetzee, A., Casini, A., Ciattini, S., Scozzafava, A., Supuran, C.T., Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the antipsychotic drug sulpiride (2004) Bioorg. Med. Chem. Lett., 14, pp. 337-341
Abbate, F., Winum, J.Y., Potter, B.V., Casini, A., Montera, J.L., Scozzafava, A., Supuran, C.T., Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with EMATE, a dual inhibitor of carbonic anhydrases and steroid sulfatase (2004) Bioorg. Med. Chem. Lett., 14, pp. 231-234
Weber, A., Casini, A., Heine, A., Kuhn, D., Supuran, C.T., Scozzafava, A., Klebe, G., Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: New pharmacological opportunities due to related binding site recognition (2004) J. Med. Chem., 47, pp. 550-557
Pastorekova, S., Casini, A., Scozzafava, A., Vullo, D., Pastorek, J., Supuran, C.T., Carbonic anhydrase inhibitors: The first selective, membrane-impermeant inhibitors targeting the tumor-associated isozyme IX (2004) Bioorg. Med. Chem. Lett., 14, pp. 869-873
Scozzafava, A., Briganti, F., Hies, 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
Casey, J.R., Morgan, P.E., Vullo, D., Scozzafava, A., Mastrolorenzo, A., Supuran, C.T., Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX (2004) J. Med. Chem., 47, pp. 2337-2347
Balaban, A.T., Dinculescu, A., Dorofeenko, G.N., Fischer, G.W., Koblik, A.V., Mezheritskii, V.V., Schroth, W., Pyrylium salts: Syntheses, reactions and physical properties (1982) Advances in Heterocyclic Chemistry, pp. 8-360. , Katritzky, A. R. (Ed.). Academic Press: New York
Supuran, C.T., Manole, G., Dinculescu, A., Schiketanz, A., Gheorghiu, M.D., Puscas, I., Balaban, A.T., Carbonic anhydrase inhibitors. V: Pyrylium salts in the synthesis of isozyme-specific inhibitors (1992) J. Pharm. Sci., 81, pp. 716-719
Khalifah, R.G., The carbon dioxide hydration activity of carbonic anhydrase (1971) J. Biol. Chem., 246, pp. 2561-2573
Brimger, A.T., Adams, P.D., Clore, G.M., De Lano, W.L., Gros, P., Grosse-Kunstleve, R.W., Jiang, J.S., Warren, G.L., Crystallography & NMR System: A new software suite for macromolecular structure determination (1998) Acta Crystallogr. Sect. D, 54, pp. 905-921
Otwinowski, Z., Minor, W., Processing of X-ray diffraction data collected in oscillation mode (1997) Methods Enzymol., 276, pp. 307-326
Jones, T.A., Zou, J.Y., Cowan, S.W., Kjeldgaard, M., Improved methods for building protein models in electron density maps and the location of errors in these models (1991) Acta Crystallogr. Sect. A, 47, pp. 110-119
Engh, R.A., Huber, R., Accurate bond and angle parameters for X-ray protein structure refinement (1991) Acta Crystallogr. Sect. A, 47, pp. 392-400
Laskowski, R.A., MacArthur, M.W., Moss, D.S., Thornton, J.M., PROCHECK: A program to check the stereochemical quality of protein structures (1993) J. Appl. Crystallogr., 26, pp. 283-291
Marquis, R. E., Whitson, J. T., Management of glaucoma: Focus on pharmacological therapy (2005) Drugs Aging, 22, pp. 1-21
Supuran, C. T., Casini, A., Scozzafava, A., Development of sulfonamide carbonic anhydrase inhibitors (CAIs) (2004) Carbonic Anhydrase - Its Inhibitors and Activators, pp. 67-148. , Supuran, C. T., Scozzafava, A., Conway, J.
Loiselle, F. B., Morgan, P. E., Alvarez, B. V., Casey, J. R., Regulation of the human NBC3 Na+/HCO3- Cotransporter by carbonic anhydrase II and PKA (2004) Am. J. Physiol. Cell Physiol., 286, pp. C1423-C1433
Lyons, K. E., Pahwa, R., Cornelia, C. L., Eisa, M. S., Elble, R. J., Fahn, S., Jankovic, J., Watts, R. L., Benefits and risks of pharmacological treatments for essential tremor (2003) Drug Saf., 26, pp. 461-481
Garske, L. A., Brown, M. G., Morrison, S. C., Acetazolamide reduces exercise capacity and increases leg fatigue under hypoxic conditions (2003) J. Appl. Physiol., 94, pp. 991-996
Winum, J. Y., Scozzafava, A., Montera, J. L., Supuran, C. T., Sulfamates and their therapeutic potential (2005) Med. Res. Rev., 25, pp. 186-228
Winum, J. Y., Pastorekova, S., Jakubickova, L., Montero, J. L., Scozzafava, A., Pastorek, J., Vullo, D., Supuran, C. T., Carbonic anhydrase inhibitors: Synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates (2005) Bioorg. Med. Chem. Lett., 15, pp. 579-584
Eriksson, A. E., Jones, T. A., Liljas, A., Refined structure of human carbonic anhydrase II at 2. 0 resolution (1988) Proteins Struct. Funct., 4, pp. 274-282
Boriack, P. A., Christianson, D. W., Kingery-Wood, J., Whitesides, G. M., Secondary interactions significantly removed from the sulfonamide binding pocket of carbonic anhydrase II influence inhibitor binding constants (1995) J. Med. Chem., 38, pp. 2286-2291
Kim, C. Y., Chandra, P. P., Jain, A., Christianson, D. W., Fluoroaromatic-fluoroaromatic interactions between inhibitors bound in the crystal lattice of human carbonic anhydrase II (2001) J. Am. Chem. Soc., 123, pp. 9620-9627
Casey, J. R., Morgan, P. E., Vullo, D., Scozzafava, A., Mastrolorenzo, A., Supuran, C. T., Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX (2004) J. Med. Chem., 47, pp. 2337-2347
Balaban, A. T., Dinculescu, A., Dorofeenko, G. N., Fischer, G. W., Koblik, A. V., Mezheritskii, V. V., Schroth, W., Pyrylium salts: Syntheses, reactions and physical properties (1982) Advances in Heterocyclic Chemistry, pp. 8-360. , Katritzky, A. R. (Ed.). Academic Press: New York
Supuran, C. T., Manole, G., Dinculescu, A., Schiketanz, A., Gheorghiu, M. D., Puscas, I., Balaban, A. T., Carbonic anhydrase inhibitors. V: Pyrylium salts in the synthesis of isozyme-specific inhibitors (1992) J. Pharm. Sci., 81, pp. 716-719
Khalifah, R. G., The carbon dioxide hydration activity of carbonic anhydrase (1971) J. Biol. Chem., 246, pp. 2561-2573
Brimger, A. T., Adams, P. D., Clore, G. M., De Lano, W. L., Gros, P., Grosse-Kunstleve, R. W., Jiang, J. S., Warren, G. L., Crystallography & NMR System: A new software suite for macromolecular structure determination (1998) Acta Crystallogr. Sect. D, 54, pp. 905-921
Jones, T. A., Zou, J. Y., Cowan, S. W., Kjeldgaard, M., Improved methods for building protein models in electron density maps and the location of errors in these models (1991) Acta Crystallogr. Sect. A, 47, pp. 110-119
Engh, R. A., Huber, R., Accurate bond and angle parameters for X-ray protein structure refinement (1991) Acta Crystallogr. Sect. A, 47, pp. 392-400
Laskowski, R. A., MacArthur, M. W., Moss, D. S., Thornton, J. M., PROCHECK: A program to check the stereochemical quality of protein structures (1993) J. Appl. Crystallogr., 26, pp. 283-291
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2005 Sep 8; 48(18): 5721-5727.
Export to Esporta in BibTeX Export to Esporta in EndNote
Paper type Tipo di articolo: Journal Article,
Impact factor: 4.926, 5-year impact factor Impact factor a 5 anni: 5.504
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-24744467784&partnerID=40&md5=1c4ee242723e3de5189fb90a3acd55d9
Keywords Parole chiave: 1 N (4 Sulfamoylphenylethyl) 2, 6 Trimethylpyridinium Perchlorate, Carbonate Dehydratase Ii, Carbonate Dehydratase Inhibitor, Carbonate Dehydratase Xii, Glutamine, Isoenzyme, Leucine, Phenylalanine, Sulfonamide, Threonine, Unclassified Drug, Valine, Amino Acid Sequence, Antineoplastic Activity, Article, Complex Formation, Crystal Structure, Drug Binding Site, Drug Structure, Hydrophilicity, Hydrophobicity, Protein Expression, Protein Targeting, Structure Analysis, X Ray Crystallography, Antigens, Antineoplastic Agents, Carbonic Anhydrase Ii, Cell Membrane Permeability, X-Ray, Humans, Models, Molecular, Molecular Structure, Protein Binding, Pyridinium Compounds, Quantitative Structure-Activity Relationship, Recombinant Proteins, Tumor Markers, Biological,
Affiliations Affiliazioni:
*** IBB - CNR ***
Istituto di Biostrutture e Bioimmagini, CNR, via Mezzocannone 16, 80134 Naples, Italy
Bioindustry Park del Canavese Spa, Via Ribes 5, 10010 Colleretto Giacosa (Torino), Italy
Dipartimento delle Scienze Biologiche, Sezione Biostrutture, University of Naples Federico II, via Mezzocannone 16, 80134 Naples, Italy
Università degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence), Italy
Universit degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence), Italy
References Riferimenti:
Supuran, C.T., Scozzafava, A., Conway, J., (2004) Carbonic Anhydrase - Its Inhibitors and Activators, pp. 1-363. , CRC Press: Boca Rato
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
Pastorekova, S., Parkkila, S., Pastorek, J., Supuran, C.T., Carbonic anhydrases: Current state of the art, therapeutic applications and future prospects (2004) J. Enzyme. Inhib. Med. Chem., 19, pp. 199-229
Marquis, R.E., Whitson, J.T., Management of glaucoma: Focus on pharmacological therapy (2005) Drugs Aging, 22, pp. 1-21
Vullo, D., Innocenti, A., Nishimori, I., Pastorek, J., Scozzafava, A., Pastorekova, S., Supuran, C.T., Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides - A new target for the design of antitumor and antiglaucoma drugs? (2005) Bioorg. Med. Chem. Lett., 15, pp. 963-969
Supuran, C.T., Casini, A., Scozzafava, A., Development of sulfonamide carbonic anhydrase inhibitors (CAIs) (2004) Carbonic Anhydrase - Its Inhibitors and Activators, pp. 67-148. , Supuran, C. T., Scozzafava, A., Conway, J.
Eds., CRC Press: Boca Raton (FL), USA
Loiselle, F.B., Morgan, P.E., Alvarez, B.V., Casey, J.R., Regulation of the human NBC3 Na+/HCO3- Cotransporter by carbonic anhydrase II and PKA (2004) Am. J. Physiol. Cell Physiol., 286, pp. C1423-C1433
Rivera, C., Voipio, J., Kaila, K., Two developmental switches in GABAergic signalling: The K+-Cl- Cotransporter KCC2 and carbonic anhydrase CAVII (2005) J. Physiol., 562, pp. 27-36
Vullo, D., Voipio, J., Innocenti, A., Rivera, C., Ranki, H., Scozzafava, A., Kaila, K., Supuran, C.T., Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides (2005) Bioorg. Med. Chem. Lett., 15, pp. 971-976
Lyons, K.E., Pahwa, R., Cornelia, C.L., Eisa, M.S., Elble, R.J., Fahn, S., Jankovic, J., Watts, R.L., Benefits and risks of pharmacological treatments for essential tremor (2003) Drug Saf., 26, pp. 461-481
Garske, L.A., Brown, M.G., Morrison, S.C., Acetazolamide reduces exercise capacity and increases leg fatigue under hypoxic conditions (2003) J. Appl. Physiol., 94, pp. 991-996
Hori, K., Ishida, S., Inoue, M., Shinoda, K., Kawashima, S., Kitamura, S., Oguchi, Y., Treatment of cystoid macular edema with oral acetazolamide in a patient with best vitelliform macular dystrophy (2004) Retina, 24, pp. 481-482
Winum, J.Y., Scozzafava, A., Montera, J.L., Supuran, C.T., Sulfamates and their therapeutic potential (2005) Med. Res. Rev., 25, pp. 186-228
Svastova, E., Hulikova, A., Rafajova, M., Zat'ovicova, M., Gibadulinova, A., Casini, A., Cecchi, A., Pastorekova, S., Hypoxia activates the capacity of tumor-associated carbonic anhydrase IX to acidify extracellular pH (2004) FEBS Lett., 577, pp. 439-445
Pastorek, J., Pastorekova, S., Callebaut, I., Mornon, J.P., Zelnik, V., Opavsky, R., Zat'ovicova, M., Stanbridge, E.J., 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
Rafajova, M., Zatovicova, M., Kettmann, R., Pastorek, J., Pastorekova, S., Induction by hypoxia combined with low glucose or low bicarbonate and high posttranslational stability upon reoxygenation contribute to carbonic anhydrase IX expression in cancer cells (2004) Int. J. Oncol., 24, pp. 995-1004
Ivanov, S., Liao, S.Y., Ivanova, A., Danilkovitch-Miagkova, A., Tarasova, N., Weirich, G., Merrill, M.J., Stanbridge, E.J., Expression of hypoxia-inducible cell-surface transmembrane carbonic anhydrases in human cancer (2001) Am. J. Pathol., 158, pp. 905-919
Winum, J.Y., Pastorekova, S., Jakubickova, L., Montero, J.L., Scozzafava, A., Pastorek, J., Vullo, D., Supuran, C.T., Carbonic anhydrase inhibitors: Synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates (2005) Bioorg. Med. Chem. Lett., 15, pp. 579-584
Vullo, D., Franchi, M., Gallon, E., Pastorek, J., Scozzafava, A., Pastorekova, S., Supuran, C.T., Carbonic anhydrase inhibitors: Inhibition of the tumor-associated isozyme IX with aromatic and heterocyclic sulfonamides (2003) Bioorg. Med. Chem. Lett., 13, pp. 1005-1009
Krungkrai, J., Scozzafava, A., Reungprapavut, S., Krungkrai, S.R., Rattanajak, R., Kamchonwongpaisan, S., Supuran, C.T., Carbonic anhydrase inhibitors. Inhibition of Plasmodium falciparum carbonic anhydrase with aromatic sulfonamides: Towards antimalarials with a novel mechanism of action? (2005) Bioorg Med. Chem., 13, pp. 483-489
Covarrubias Suarez, A., Larsson, A.M., Ho Gbom, M., Lindberg, J., Bergfors, T., Bjo Rkelid, C., Mowbray, S.L., Jones, T.A., Structure and function of carbonic anhydrases from mycobacterium tuberculosis (2005) J. Biol. Chem., 280, pp. 18782-18789
Chakravarty, S., Kannan, K.K., Drug-protein interactions. Refined structures of three sulfonamide drug complexes of human carbonic anhydrase I enzyme (1994) J. Mol. Biol., 243, pp. 298-309
Vidgren, J., Svensson, A., Liljas, A., Refined structure of the aminobenzolamide complex of human carbonic anhydrase II at 1.9 A and sulphonamide modelling of bovine carbonic anhydrase III (1993) Int. J. Biol. Macromol., 15, pp. 97-100
Eriksson, A.E., Jones, T.A., Liljas, A., Refined structure of human carbonic anhydrase II at 2.0 Å resolution (1988) Proteins Struct. Funct., 4, pp. 274-282
Boriack, P.A., Christianson, D.W., Kingery-Wood, J., Whitesides, G.M., Secondary interactions significantly removed from the sulfonamide binding pocket of carbonic anhydrase II influence inhibitor binding constants (1995) J. Med. Chem., 38, pp. 2286-2291
Stams, T., Chen, Y., Boriack-Sjodin, P.A., Hurt, J.D., Liao, J., May, J.A., Dean, T., Christianson, D.W., Structures of murine carbonic anhydrase IV and human carbonic anhydrase II complexed with brinzolamide: Molecular basis of isozyme-drug discrimination (1998) Protein Sci., 7, pp. 556-563
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Di Fiore, A., De Simone, G., Menchise, V., Pedone, C., Casini, A., Scozzafava, A., Supuran, C.T., 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 (2005) Bioorg. Med. Chem. Lett., 15, pp. 1937-1942
Abbate, F., Casini, A., Scozzafava, A., Supuran, C.T., Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the perfluorobenzoyl analogue of methazolamide. Implications for the drug design of fluorinated inhibitors (2003) J. Enzyme. Inhib. Med. Chem., 18, pp. 303-308
Casini, A., Abbate, F., Scozzafava, A., Supuran, C.T., Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with a bis-sulfonamide-two heads are better than one? (2003) Bioorg. Med. Chem. Lett., 13, pp. 2759-2763
Casini, A., Antel, J., Abbate, F., Scozzafava, A., David, S., Waldeck, H., Schafer, S., Supuran, C.T., Carbonic anhydrase inhibitors: SAR and X-ray crystallographic study for the interaction of sugar sulfamates/sulfamides with isozymes I, II and IV (2003) Bioorg. Med. Chem. Lett., 13, pp. 841-845
Abbate, F., Coetzee, A., Casini, A., Ciattini, S., Scozzafava, A., Supuran, C.T., Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the antipsychotic drug sulpiride (2004) Bioorg. Med. Chem. Lett., 14, pp. 337-341
Abbate, F., Winum, J.Y., Potter, B.V., Casini, A., Montera, J.L., Scozzafava, A., Supuran, C.T., Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with EMATE, a dual inhibitor of carbonic anhydrases and steroid sulfatase (2004) Bioorg. Med. Chem. Lett., 14, pp. 231-234
Weber, A., Casini, A., Heine, A., Kuhn, D., Supuran, C.T., Scozzafava, A., Klebe, G., Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: New pharmacological opportunities due to related binding site recognition (2004) J. Med. Chem., 47, pp. 550-557
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Kim, C. Y., Chandra, P. P., Jain, A., Christianson, D. W., Fluoroaromatic-fluoroaromatic interactions between inhibitors bound in the crystal lattice of human carbonic anhydrase II (2001) J. Am. Chem. Soc., 123, pp. 9620-9627
Casey, J. R., Morgan, P. E., Vullo, D., Scozzafava, A., Mastrolorenzo, A., Supuran, C. T., Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX (2004) J. Med. Chem., 47, pp. 2337-2347
Balaban, A. T., Dinculescu, A., Dorofeenko, G. N., Fischer, G. W., Koblik, A. V., Mezheritskii, V. V., Schroth, W., Pyrylium salts: Syntheses, reactions and physical properties (1982) Advances in Heterocyclic Chemistry, pp. 8-360. , Katritzky, A. R. (Ed.). Academic Press: New York
Supuran, C. T., Manole, G., Dinculescu, A., Schiketanz, A., Gheorghiu, M. D., Puscas, I., Balaban, A. T., Carbonic anhydrase inhibitors. V: Pyrylium salts in the synthesis of isozyme-specific inhibitors (1992) J. Pharm. Sci., 81, pp. 716-719
Khalifah, R. G., The carbon dioxide hydration activity of carbonic anhydrase (1971) J. Biol. Chem., 246, pp. 2561-2573
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Engh, R. A., Huber, R., Accurate bond and angle parameters for X-ray protein structure refinement (1991) Acta Crystallogr. Sect. A, 47, pp. 392-400
Laskowski, R. A., MacArthur, M. W., Moss, D. S., Thornton, J. M., PROCHECK: A program to check the stereochemical quality of protein structures (1993) J. Appl. Crystallogr., 26, pp. 283-291
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
Structure for the adduct of carbonic anhydrase II with 1-N-(4- sulfamoylphenyl-ethyl)-2,4,6-trimethylpyridinium perchlorate, a membrane-impermeant antitumor sulfonamide, is reported. The phenylethyl moiety fills the active site, making van der Waals interactions with side chains of Gln192, Val121, Phe131, Leu198, Thr200. The 2,4,6-trimethylpyridinium functionality is at van der Waals distance from the aliphatic chain of Ile91 being involved in strong offset face-to-face stacking with Phe131. Analyzing X-ray crystal structures of such adducts, two binding modes were observed: some inhibitors bind with their tail within the hydrophobic half of the active site, defined by residues Phe131, Val135, Leu198, Pro202, Leu204. Other derivatives bind with their tail in a different region, pointing toward the hydrophilic half and making strong parallel stacking with Phe131. This interaction orients the inhibitor toward the hydrophilic part of the active site. Impossibility to participate in it leads to its binding within the hydrophobic half. Such findings are relevant for designing better inhibitors targeting isozymes II, IX, and XII, some of which are overexpressed in hypoxic tumors. © 2005 American Chemical Society.
Structure for the adduct of carbonic anhydrase II with 1-N-(4- sulfamoylphenyl-ethyl)-2,4,6-trimethylpyridinium perchlorate, a membrane-impermeant antitumor sulfonamide, is reported. The phenylethyl moiety fills the active site, making van der Waals interactions with side chains of Gln192, Val121, Phe131, Leu198, Thr200. The 2,4,6-trimethylpyridinium functionality is at van der Waals distance from the aliphatic chain of Ile91 being involved in strong offset face-to-face stacking with Phe131. Analyzing X-ray crystal structures of such adducts, two binding modes were observed: some inhibitors bind with their tail within the hydrophobic half of the active site, defined by residues Phe131, Val135, Leu198, Pro202, Leu204. Other derivatives bind with their tail in a different region, pointing toward the hydrophilic half and making strong parallel stacking with Phe131. This interaction orients the inhibitor toward the hydrophilic part of the active site. Impossibility to participate in it leads to its binding within the hydrophobic half. Such findings are relevant for designing better inhibitors targeting isozymes II, IX, and XII, some of which are overexpressed in hypoxic tumors. © 2005 American Chemical Society.
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
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
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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 (410 visite)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2012; 55(15): 6776-6783.
Impact Factor: 5.614
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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 (320 visite)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2012; 48(70): 8838-8840.
Impact Factor: 6.378
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Castellano I, Merlino A
* γ-glutamyltranspeptidases: Sequence, structure, biochemical properties, and biotechnological applications (363 visite)
Cell Mol Life Sci (ISSN: 1420-682x), 2012; 69(20): 3381-3394.
Impact Factor: 5.615
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Diana D, Basile A, De Rosa L, Di Stasi R, Auriemma S, Arra C, Pedone C, Turco MC, Fattorusso R, D'Andrea LD
* Beta-Hairpin Peptide That Targets Vascular Endothelial Growth Factor (vegf) Receptors: Design, Nmr Characterization, And Biological Activity (516 visite)
Jbc Papers (ISSN: 1083-351x, 0021-9258, 0021-9258linking), 2011 Dec 2; 286(48): 41680-41691.
Impact Factor: 4.773
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Scognamiglio PL, Doti N, Grieco P, Pedone C, Ruvo M, Marasco D
* Discovery Of Small Peptide Antagonists Of Ped/Pea15-D4alpha Interaction From Simplified Combinatorial Libraries (431 visite)
Chem Biol Drug Des Chemical Biology And Drug Design (ISSN: 1747-0277, 1747-0285), 2011 May; 77(5): 319-327.
Impact Factor: 2.282
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Basile A, Del Gatto A, Diana D, Di Stasi R, Falco A, Festa M, Rosati A, Barbieri A, Franco R, Arra C, Pedone C, Fattorusso R, Turco MC, D'Andrea LD
* Characterization of a designed vascular endothelial growth factor receptor antagonist helical peptide with antiangiogenic activity in vivo (425 visite)
J Med Chem (ISSN: 1520-4804, 0022-2623, 0022-2623print), 2011 Mar 10; 54(5): 1391-1400.
Impact Factor: 5.248
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Accardo A, Morisco A, Gianolio E, Tesauro D, Mangiapia G, Radulescu A, Brandt A, Morelli G
* Nanoparticles containing octreotide peptides and gadolinium complexes for MRI applications (456 visite)
J Pept Sci (ISSN: 1075-2617, 1099-1387, 1075-2617print), 2011 Feb; 17(2): 154-162.
Impact Factor: 1.799
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Milardi D, Sciacca MFM, Pappalardo M, Grasso DM, La Rosa C
* The Role Of Aromatic Side-Chains In Amyloid Growth And Membrane Interaction Of The Islet Amyloid Polypeptide Fragment Lanflvh (373 visite)
Eur Biophys J, 2011 Jan; 40(1): 1-12.
Impact Factor: 3.832
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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 (317 visite)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2011; 47(42): 11636-11638.
Impact Factor: 6.169
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Castellano I, Di Salle A, Merlino A, Rossi M, La Cara F
* Gene cloning and protein expression of γ-glutamyltranspeptidases from Thermus thermophilus and Deinococcus radiodurans: Comparison of molecular and structural properties with mesophilic counterparts (285 visite)
Extremophiles (ISSN: 1431-0651, 1433-4909, 1433-4909electronic), 2011; 15(2): 259-270.
Impact Factor: 2.941
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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 (299 visite)
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 (365 visite)
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, 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 (313 visite)
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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Pensato S, Renda M, Leccia F, Saviano M, D'Andrea LD, Pedone C, Pedone PV, Romanelli A
* PNA zipper as a dimerization tool: development of a bZip mimic (446 visite)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 2010 May; 93(5): 434-441.
Impact Factor: 2.572
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Bruni AC, Bernardi L, Colao R, Rubino E, Smirne N, Frangipane F, Terni B, Curcio SA, Mirabelli M, Clodomiro A, Di Lorenzo R, Maletta R, Anfossi M, Gallo M, Geracitano S, Tomaino C, Muraca MG, Leotta A, Lio SG, Pinessi L, Rainero I, Sorbi S, Nee L, Milan G, Pappata S, Postiglione A, Abbamondi N, Forloni G, St George Hyslop P, Rogaeva E, Bugiani O, Giaccone G, Foncin JF, Spillantini MG, Puccio G
* Worldwide distribution of PSEN1 Met146Leu mutation: A large variability for a founder mutation (506 visite)
Neurology (ISSN: 0028-3878, 1526-632x, 1526-632xelectronic), 2010 Mar 9; 74(10): 798-806.
Impact Factor: 8.017
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De Simone G, Supuran CT
* Carbonic anhydrase IX: Biochemical and crystallographic characterization of a novel antitumor target (357 visite)
Bba-Gen Subjects (ISSN: 1570-9639, 0006-3002, 0925-4439), 2010 Feb; 1804(2): 404-409.
Impact Factor: 2.773
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Sciacca MFM, Pappalardo M, Attanasio F, Milardi D, La Rosa C, Grasso DM
* Are fibril growth and membrane damage linked processes? An experimental and computational study of IAPP(12-18) and IAPP(21-27) peptides (377 visite)
New J Chem (ISSN: 1144-0546), 2010; 34(2): 200-207.
Impact Factor: 2.631
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Guler OO, De Simone G, Supuran CT
* Drug design studies of the novel antitumor targets carbonic anhydrase IX and XII (437 visite)
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 (401 visite)
Curr Pharm Des Current Pharmaceutical Design (ISSN: 1381-6128, 1873-4286), 2010; 16(29): 3246-3254.
Impact Factor: 4.774
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Merlino A, Russo Krauss I, Perillo M, Mattia CA, Ercole C, Picone D, Vergara A, Sica F
* Toward an Antitumor Form of Bovine Pancreatic Ribonuclease: The Crystal Structure of Three Noncovalent Dimeric Mutants (361 visite)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 2009 Dec; 91(12): 1029-1037.
Impact Factor: 2.605
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Farina AR, Tacconelli A, Cappabianca L, Cea G, Chioda A, Romanelli A, Pensato S, Pedone C, Gulino A, Mackay AR
* The neuroblastoma tumour-suppressor TrkAI and its oncogenic alternative TrkAIII splice variant exhibit geldanamycin-sensitive interactions with Hsp90 in human neuroblastoma cells (344 visite)
Oncogene (ISSN: 1476-5594, 0950-9232), 2009 Nov 19; 28(46): 4075-4094.
Impact Factor: 7.135
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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 (393 visite)
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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De Simone G, Scozzafava A, Supuran CT
* Which Carbonic Anhydrases are Targeted by the Antiepileptic Sulfonamides and Sulfamates? (304 visite)
Chem Biol Drug Des Chemical Biology And Drug Design (ISSN: 1747-0277, 1747-0285), 2009 Sep; 74(3): 317-321.
Impact Factor: 2.473
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Imbriaco M, Pisani A, Spinelli L, Cuocolo A, Messalli G, Capuano E, Marmo M, Liuzzi R, Visciano B, Cianciaruso B, Salvatore M
* Effects of enzyme-replacement therapy in patients with Anderson-Fabry disease: a prospective long-term cardiac magnetic resonance imaging study (304 visite)
Heart (ISSN: 1355-6037, 1468-201x), 2009 Jul; 95(13): 1103-1107.
Impact Factor: 5.385
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De Rosa A, Criscuolo C, Mancini P, De Martino M, Giordano IA, Pappata S, Filla A, De Michele G
* Genetic screening for LRRK2 gene G2019S mutation in Parkinson's disease patients from Southern Italy (227 visite)
Parkinsonism Relat D (ISSN: 1353-8020print, 1353-8020linking, 1873-5126electronic), 2009 Mar; 15(3): 242-244.
Impact Factor: 2.406
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Kaczmarek K, Farina B, Zubrzak P, Jankowski S, Zimecki M, Suder P, Benedetti E, Fattorusso R, Saviano M, Zabrocki J
* Synthesis, conformational analysis and immunological activity of β3Phe-substituted Cyclolinopeptide A analogues (436 visite)
J Pept Sci (ISSN: 1075-2617, 1099-1387, 1075-2617print), 2009 Mar; 15(3): 166-174.
Impact Factor: 1.807
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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 (409 visite)
Proteins (ISSN: 1097-0134, 0887-3585, 1097-0134electronic), 2009 Jan; 74(1): 164-175.
Impact Factor: 3.085
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Merlino A, Avella G, Di Gaetano S, Arciello A, Piccoli R, Mazzarella L, Sica F
* Structural features for the mechanism of antitumor action of a dimeric human pancreatic ribonuclease variant (323 visite)
Protein Sci (ISSN: 0961-8368, 1469-896xelectronic, 0961-8368linking), 2009 Jan; 18(1): 50-57.
Impact Factor: 2.937
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Pentimalli F, Palmieri D, Pacelli R, Garbi C, Cesari R, Martin E, Pierantoni GM, Chieffi P, Croce CM, Costanzo V, Fedele M, Fusco A
* HMGA1 protein is a novel target of the ATM kinase (433 visite)
European Journal Of Cancer (ISSN: 0959-8049), 2008 Nov; 44(17): 2668-2679.
Impact Factor: 4.475
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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 (384 visite)
Jbc Papers (ISSN: 0021-9258, 1083-351x, 0021-9258linking), 2008 Oct 10; 283(41): 27799-27809.
Impact Factor: 5.52
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Dudar GK, D'Andrea LD, Di Stasi R, Pedone C, Wallace JL
* A vascular endothelial growth factor mimetic accelerates gastric ulcer healing in an iNOS-dependent manner (635 visite)
Am J Physiol Gastrointest Liver Physiol American Journal Of Physiology Gastrointestinal And Liver Physiology (ISSN: 0193-1857), 2008 Sep; 295(2): G374-G381.
Impact Factor: 3.587
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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 (443 visite)
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 (414 visite)
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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Esposito L, Paladino A, Pedone C, Vitagliano L
* Insights into structure, stability, and toxicity of monomeric and aggregated polyglutamine models from molecular dynamics simulations (315 visite)
Biophysical Journal (ISSN: 1542-0086, 0006-3495), 2008 May 15; 94(10): 4031-4040.
Impact Factor: 4.683
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Rendina D, De Filippo G, Viceconti R, Soscia E, Sirignano C, Salvatore M, Della Monica M, Scarano G, Mossetti G
* Interleukin (il)-6 And Receptor Activator Of Nuclear Factor (nf)-Kappab Ligand (rankl) Are Increased In The Serum Of A Patient With Primary Pachydermoperiostosis (411 visite)
Scand J Rheumatol (ISSN: 0300-9742), 2008 May; 37(3): 225-229.
Impact Factor: 2.345
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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 (361 visite)
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 (339 visite)
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 (386 visite)
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? (361 visite)
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 (333 visite)
Chemmedchem (ISSN: 1860-7179, 1860-7187, 1860-7187electronic), 2008 Mar; 3(3): 473-477.
Impact Factor: 3.15
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Merlino A, Ercole C, Picone D, Pizzo E, Mazzarella L, Sica F
* The buried diversity of bovine seminal ribonuclease: Shape and cytotoxicity of the swapped non-covalent form of the enzyme (350 visite)
J Mol Biol (ISSN: 0022-2836, 1089-8638, 1089-8638electronic), 2008 Feb 15; 376(2): 427-437.
Impact Factor: 4.146
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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 (332 visite)
Curr Pharm Des Current Pharmaceutical Design (ISSN: 1381-6128, 1873-4286), 2008; 14(7): 672-678.
Impact Factor: 4.399
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Giordano D, Vergara A, Lee HC, Peisach J, Balestrieri M, Mazzarella L, Parisi E, Di Priseo G, Verde C
* Hemoglobin structure/function and globin-gene evolution in the Arctic fish Liparis tunicatus (331 visite)
Gene (ISSN: 0378-1119), 2007 Dec 30; 406(1-2): 58-68.
Impact Factor: 2.871
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Calabrese V, Mancuso C, Calvani M, Rizzarelli E, Butterfield DA, Stella AM
* Nitric oxide in the central nervous system: neuroprotection versus neurotoxicity (494 visite)
Nature Reviews Neuroscience (ISSN: 1471-0048), 2007 Oct; 8(10): 766-775.
Impact Factor: 24.52
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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 (304 visite)
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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De Rosa A, Carducci C, Antonozzi I, Giovanniello T, Xhoxhi E, Criscuolo C, Menchise V, Striano S, Filla A, De Michele G
* A novel mutation in GCH-1 gene in a case of dopa-responsive dystonia [9] (288 visite)
J Neurol (ISSN: 0340-5354, 1432-1459, 1432-1459electronic), 2007 Sep; 254(8): 1133-1134.
Impact Factor: 2.477
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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 (311 visite)
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 (389 visite)
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 (396 visite)
Curr Top Med Chem (ISSN: 1568-0266, 1568-0266linking, 1873-4294electronic), 2007; 7(9): 879-884.
Impact Factor: 4.325
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Cucinotta V, Giuffrida A, Grasso G, Maccarrone G, Messina M, Vecchio G
* High selectivity in new chiral separations of dansyl amino acids by cyclodextrin derivatives in electrokinetic chromatography (260 visite)
J Chromatogr A (ISSN: 0021-9673), 2007; 1155(2): 172-179.
Impact Factor: 3.641
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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 (799 visite)
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 (280 visite)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2006 Dec 15; 16(24): 6204-6208.
Impact Factor: 2.538
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Pailot A, D'Ambrosio K, Corbier C, Talfournier F, Branlant G
* Invariant Thr(244) is essential for the efficient acylation step of the non-phosphorylating glyceraldehyde-3-phosphate dehydrogenase from Streptococcus mutans (301 visite)
Biochem J (ISSN: 0264-6021, 1470-8728electronic, 0264-6021linking), 2006 Dec 15; 400: 521-530.
Impact Factor: 4.1
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Saporito A, Marasco D, Chambery A, Botti P, Monti SM, Pedone C, Ruvo M
* The chemical synthesis of the GstI protein by NCL on a X-Met site (584 visite)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 2006 Dec 5; 83(5): 508-518.
Impact Factor: 2.48
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Dalla Bona A, Formaggio F, Peggion C, Kaptein B, Broxterman Quirinus B, Galdiero S, Galdiero M, Vitiello M, Benedetti E, Toniolo C
* Synthesis, conformation, and bioactivity of novel analogues of the antiviral lipopeptide halovir (427 visite)
J Pept Sci (ISSN: 1075-2617, 1099-1387, 1075-2617print), 2006 Dec; 12(12): 748-757.
Impact Factor: 1.801
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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 (417 visite)
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 (374 visite)
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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Merlino A, Esposito L, Vitagliano L
* Polyglutamine Repeats And Beta-Helix Structure: Molecular Dynamics Study (466 visite)
Proteins (ISSN: 0887-3585, 1097-0134, 1097-0134electronic), 2006 Jun 1; 63(4): 918-927.
Impact Factor: 3.73
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Mazzarella L, Bonomi G, Lubrano MC, Merlino A, Riccio A, Vergara A, Vitagliano L, Verde C, Di Prisco G
* Minimal structural requirements for root effect: Crystal structure of the cathodic hemoglobin isolated from the Antarctic fish Trematomus newnesi (447 visite)
Proteins (ISSN: 0887-3585, 1097-0134, 1097-0134electronic), 2006 Feb 1; 62(2): 316-321.
Impact Factor: 3.73
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D'Andrea LD, Del Gatto A, Pedone C, Benedetti E
* Peptide-based molecules in angiogenesis (612 visite)
Chem Biol Drug Des (ISSN: 1747-0277, 1747-0285, 1747-0277linking), 2006 Feb; 67(2): 115-126.
Impact Factor: 2.507
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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 (292 visite)
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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Iaccarino G, Izzo R, Trimarco V, Cipolletta E, Lanni F, Sorriento D, Iovino GL, Rozza F, De Luca N, Priante O, Di Renzo G, Trimarco B
* β 2-Adrenergic receptor polymorphisms and treatment-induced regression of left ventricular hypertrophy in hypertension (337 visite)
Clin Pharmacol Ther Clinical Pharmacology And Therapeutics (ISSN: 0009-9236), 2006; 80(6): 633-645.
Impact Factor: 8.066
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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 (306 visite)
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 (436 visite)
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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Esposito G, Vitagliano L, Cevenini A, Amelio T, Zagari A, Salvatore F
* Unraveling the structural and functional features of an aldolase A mutant involved in the hemolytic anemia and severe rhabdomyolysis reported in a child (311 visite)
Haematologica (ISSN: 0006-4971, 0006-6497, 0390-6078), 2005 Jan 15; 105(2): 905-906.
Impact Factor: 10.131
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Zubrzak P, Banas A, Kaczmarek K, Leplawy MT, Sochacki M, Kowalski ML, Szkudlinska B, Zabrocki J, Di Lello P, Isernia C, Saviano M, Pedone C, Benedetti E
* Analogues of cyclolinopeptide A containing alpha-hydroxymethyl amino acid residues (423 visite)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 2005; 80(2-3): 347-356.
Impact Factor: 2.425
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Merlino A, Graziano G, Mazzarella L
* Structural And Dynamic Effects Of Alpha-Helix Deletion In Sso7d: Implications For Protein Thermal Stability (325 visite)
Proteins (ISSN: 0887-3585, 1097-0134, 1097-0134electronic), 2004 Dec 1; 57(4): 692-701.
Impact Factor: 4.429
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Borgatti M, Finotti A, Romanelli A, Saviano M, Bianchi N, Lampronti I, Lambertini E, Penolazzi L, Nastruzzi C, Mischiati C, Piva R, Pedone C, Gambari R
* Peptide nucleic acids (PNA)-DNA chimeras targeting transcription factors as a tool to modify gene expression (452 visite)
Curr Drug Targets (ISSN: 1389-4501), 2004 Nov; 5(8): 735-744.
Impact Factor: 4.104
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Bonomo RP, Castronovo BM, Santoro AM
* A Spectroscopic Investigation Of The Interaction Between Nitrogen Monoxide And Copper Sites Of The Fungal Laccase From Rigidoporus Lignosus (260 visite)
Dalton Trans, 2004 Jan 7; N/D: 104-112.
Impact Factor: 4.097
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Russo M, Palumbo R, Mupo A, Tosto M, Iacomino G, Scognamiglio A, Tedesco I, Galano G, Russo GL
* Flavonoid quercetin sensitizes a CD95-resistant cell line to apoptosis by activating protein kinase Cα (334 visite)
Oncogene (ISSN: 0950-9232, 1476-5594), 2003; 22(21): 3330-3342.
Impact Factor: 6.495
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Orru S, Ruoppolo M, Francese S, Vitagliano L, Marino G, Esposito C
* Identification of tissue transglutaminase-reactive lysine residues in glyceraldehyde-3-phosphate dehydrogenase (9741 visite)
Protein Sci (ISSN: 0961-8368, 1469-896xelectronic), 2002 Jan; 11(1): 137-146.
Impact Factor: 3.546
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Garzillo AM, Colao MC, Buonocore V, Oliva R, Falcigno L, Saviano M, Santoro AM, Zappala R, Bonomo RP, Bianco C, Giardina P, Palmieri G, Sannia G
* Structural and kinetic characterization of native laccases from Pleurotas ostreatus, Rigidoporus lignosus, and Trametes trogii (347 visite)
Journal Of Protein Chemistry (ISSN: 0277-8033), 2001 Apr; 20(3): 191-201.
Impact Factor: 1.021
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Romanelli A, Garella I, Menchise V, Iacovino R, Saviano M, Montesarchio D, Didierjean C, Lello PD, Rossi F, Benedetti E
* Crystal-state conformation of Cα, α-dialkylated peptides containing chiral β-homo-residues (399 visite)
J Pept Sci (ISSN: 1075-2617, 1099-1387, 1075-2617print), 2001; 7(1): 15-26.
Impact Factor: 1.451
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De Simone G, Galdiero S, Manco G, Lang D, Rossi M, Pedone C
A snapshot of a transition state analogue of a novel thermophilic esterase belonging to the subfamily of mammalian hormone-sensitive lipase (400 visite)
J Mol Biol (ISSN: 0022-2836, 1089-8638, 1089-8638electronic), 2000 Nov 10; 303(5): 761-771.
Impact Factor: 5.388
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Esposito L, Vitagliano L, Sica F, Sorrentino G, Zagari A, Mazzarella L
The ultrahigh resolution crystal structure of ribonuclease A containing an isoaspartyl residue: Hydration and sterochemical analysis (389 visite)
J Mol Biol (ISSN: 0022-2836, 1089-8638, 1089-8638electronic), 2000 Mar 31; 297(3): 713-732.
Impact Factor: 5.388
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Oliva R, Falcigno L, D'Auria G, Zanotti G, Paolillo L
Conformation and calcium-binding properties of a bicyclic nonapeptide (326 visite)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 2000; 56(1): 27-36.
Impact Factor: 2.405
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Bonomo RP, Boudet AM, Cozzolino R, Rizzarelli E, Santoro AM, Sterjiades R, Zappalà R
A comparative study of two isoforms of laccase secreted by the 'white- rot' fungus Rigidoporus lignosus, exhibiting significant structural and functional differences (274 visite)
J Chem Res (ISSN: 0162-0134, 1873-3344, 0162-0134print), 1998 Sep; 71(3-4): 205-211.
Impact Factor: 1.162
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Arena G, Conato C, Contino A, Pulidori F, Purrello R, Remelli M, Tabbì G
Cu(II)-L-glutamine and L-asparagine binary complexes. A thermodynamic and spectroscopic study (277 visite)
Ann Chim (ISSN: 0003-4592), 1998 Jan; 88(1-2): 1-12.
Impact Factor: 0.811
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Benedetti E, Iacovino R, Pedone C, Rossi F, Saviano M, Isernia C, Montesarchio D, DeNapoli L, Piccialli G
β-Amino acid residues: Conformational characterization of an N- and C-protected homo-β-(S)-leucine (273 visite)
Int J Pept Res Ther (ISSN: 0929-5666, 1573-3149), 1997 Jun; 4(3): 129-134.
Impact Factor: 0.557
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Brunetti A, Alfano B, Soricelli A, Tedeschi E, Mainolfi C, Covelli EM, Aloj L, Panico M, Bazzicalupo L, Salvatore M
Functional characterization of brain tumors: An overview of the potential clinical value (477 visite) (PDF 227 visite)
Nucl Med Biol (ISSN: 0969-8051, 0883-2897), 1996 Sep; 23(6): 699-715.
Impact Factor: 1.042
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Pacelli R, Wink DA, Cook JA, Krishna MC, DeGraff W, Friedman N, Tsokos M, Samuni A, Mitchell JB
NITRIC-OXIDE POTENTIATES HYDROGEN PEROXIDE-INDUCED KILLING OF ESCHERICHIA-COLI (409 visite)
Journal Of Experimental Medicine (ISSN: 0022-1007), 1995 Nov 1; 182(5): 1469-1479.
Impact Factor: 14.384
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Di Blasio B, Saviano M, Del Duca V, De Simone G, Rossi F, Pedone C, Benedetti E, Lorenzi GP
CONFORMATIONAL STUDIES OF HETEROCHIRAL PEPTIDES WITH DIASTEREOISOMERIC RESIDUES - CRYSTAL AND MOLECULAR-STRUCTURES OF LINEAR DIPEPTIDES DERIVED FROM LEUCINE, ISOLEUCINE, AND ALLO-ISOLEUCINE (380 visite)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1995 Oct; 36(4): 401-408.
Impact Factor: 2.425
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Di Blasio B, Pavone V, Nastri F, Isernia C, Saviano M, Pedone C, Cucinotta V, Impellizzeri G, Rizzarelli E, Vecchio G
Conformation for a β-cyclodextrin monosubstituted with a cyclic dipeptide (430 visite)
P Natl Acad Sci Usa (ISSN: 0027-8424, 1091-6490, 0027-8424print), 1992 Sep 1; 89(15): 7218-7221.
Impact Factor: 9.04
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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 (221 visite)
Chem Commun (ISSN: 1364-548xelectronic, 1359-7345linking), 2018 Sep 11; 54(73): 10312-10315.
Impact Factor: 6.169
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Roux C, Riganti C, Borgogno SF, Curto R, Curcio C, Catanzaro V, Digilio G, Padovan S, Puccinelli MP, Isabello M, Aime S, Cappello P, Novelli F
* Endogenous glutamine decrease is associated with pancreatic cancer progression (189 visite)
Oncotarget (ISSN: 1949-2553electronic, 1949-2553linking), 2017 Aug 24; 8(56): 95361-95376.
Impact Factor: 5.008
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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 (354 visite)
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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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 (336 visite)
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 (257 visite)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391), 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 (277 visite)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391), 2017 Jan 15; pii:S0968-0896(16): 539-544.
Impact Factor: 2.881
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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 (221 visite)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391), 2017; 25(2): 539-544.
Impact Factor: 2.881
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Troise AD, Buonanno M, Fiore A, Monti SM, Fogliano V
* Evolution of protein bound Maillard reaction end-products and free Amadori compounds in low lactose milk in presence of fructosamine oxidase (293 visite)
Food Chem (ISSN: 0308-8146, 0308-8146print), 2016 Dec 1; 212: 722-729.
Impact Factor: 4.529
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La Mendola D, Arnesano F, Hansson O, Giacomelli C, Calo V, Mangini V, Magrì A, Bellia F, Trincavelli ML, Martini C, Natile G, Rizzarelli E
* Copper binding to naturally occurring, lactam form of angiogenin differs from that to recombinant protein, affecting their activity (315 visite)
Metallomics (ISSN: 1756-5901, 1756-591x), 2016 Jan 20; 8(1): 118-124.
Impact Factor: 3.975
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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 (260 visite)
J Enzyme Inhib Med Chem, 2016; 17: 1-6.
Impact Factor: 3.428
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Monti SM, Supuran CT, De Simone G
* DPP-4 inhibitors: a patent review (2012 - 2014) (341 visite)
Expert Opin Ther Pat (ISSN: 1354-3776, 1744-7674electronic), 2015 Feb; 25(2): 209-236.
Impact Factor: 4.626
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Balasco N, Barone D, Vitagliano L
* Structural conversion of the transformer protein RfaH: new insights derived from protein structure prediction and molecular dynamics simulations (347 visite)
J Biomol Struct Dyn (ISSN: 0739-1102, 1538-0254electronic, 0739-1102linking), 2015 Jan 12; 33(10): 2173-2179.
Impact Factor: 2.3
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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 (345 visite) (PDF 229 visite)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2015 Jan 7; 51(2): 302-305.
Impact Factor: 6.567
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Troise AD, Fiore A, Roviello GN, Monti SM, Fogliano V
* Simultaneous quantification of amino acids and Amadori products in foods through ion-pairing liquid chromatography-high-resolution mass spectrometry (458 visite)
Amino Acids (ISSN: 0939-4451, 1438-2199, 1438-2199electronic), 2015 Jan; 47(1): 111-124.
Impact Factor: 3.196
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Caporale A, Selis F, Pain D, Sandomenico A, Jotti S, Tonon G, Ruvo M
* The LQSP tetrapeptide is a new highly efficient substrate of microbial transglutaminase for the site-specific derivatization of peptides and proteins (432 visite)
Biotechnol J (ISSN: 1860-6768), 2015 Jan; 10(1): 154-161.
Impact Factor: 3.781
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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 (330 visite)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391), 2015; 23(15): 4181-4187.
Impact Factor: 2.923
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Braccini L, Ciraolo E, Campa CC, Perino A, Longo DL, Tibolla G, Pregnolato M, Cao Y, Tassone B, Damilano F, Laffargue M, Calautti E, Falasca M, Norata GD, Backer JM, Hirsch E
* PI3K-C2γ 3 is a Rab5 effector selectively controlling endosomal Akt2 activation downstream of insulin signalling (201 visite)
Nat Commun (ISSN: 2041-1723, 2041-1723electronic), 2015; 6: N/D-N/D.
Impact Factor: 11.329
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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 (381 visite)
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 (412 visite)
Int J Mol Sc (ISSN: 1422-0067, 1661-6596, 1422-0067linking), 2015; 16(7): 15456-15480.
Impact Factor: 3.257
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Messori L, Cinellu MA, Merlino A
* Protein Recognition of Gold-Based Drugs: 3D Structure of the Complex Formed When Lysozyme Reacts with Aubipy(c) (292 visite)
Acs Med Chem Lett (ISSN: 1948-5875), 2014 Jul 31; 5(10): 1110-1113.
Impact Factor: 3.12
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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" (351 visite)
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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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 (374 visite)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 2014; 101(7): 769-778.
Impact Factor: 2.385
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Sica F, Pica A, Merlino A, Russo Krauss I, Ercole C, Picone D
* The multiple forms of bovine seminal ribonuclease: Structure and stability of a C-terminal swapped dimer (288 visite)
Febs Lett (ISSN: 0014-5793, 0014-5793print, 1873-3468electronic), 2013 Nov 29; 587(23): 3755-3762.
Impact Factor: 3.341
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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 (478 visite)
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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McNeill A, Wu RM, Tzen KY, Aguiar PC, Arbelo JM, Barone P, Bhatia K, Barsottini O, Bonifati V, Bostantjopoulou S, Bressan R, Cossu G, Cortelli P, Felicio A, Ferraz HB, Herrera J, Houlden H, Hoexter M, Isla C, Lees A, Lorenzo-Betancor O, Mencacci NE, Pastor P, Pappata S, Pellecchia MT, Silveria-Moriyama L, Varrone A, Foltynie T, Schapira AH
* Dopaminergic Neuronal Imaging in Genetic Parkinson's Disease: Insights into Pathogenesis (415 visite)
Plosone (ISSN: 1932-6203, 1932-6203electronic), 2013 Jul 23; 8(7): e69190-e69190.
Impact Factor: 3.534
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De Simone G, Alterio V, Supuran CT
* Exploiting the hydrophobic and hydrophilic binding sites for designing carbonic anhydrase inhibitors (382 visite)
Expert Opin Drug Discov (ISSN: 1746-0441), 2013 Jul; 8(7): 793-810.
Impact Factor: 3.467
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Monti SM, Supuran CT, De Simone G
* Anticancer carbonic anhydrase inhibitors: A patent review (2008-2013) (383 visite)
Expert Opin Ther Pat (ISSN: 1354-3776, 1744-7674electronic), 2013 Jun; 23(6): 737-749.
Impact Factor: 3.441
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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? (391 visite)
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 (348 visite)
J Chem Res (ISSN: 0162-0134, 1873-3344, 0162-0134print), 2012 Jun; 111: 117-129.
Impact Factor: 3.197
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Bucci M, Cigliano L, Vellecco V, D'Andrea LD, Ziaco B, Rossi A, Sautebin L, Carlucci A, Abrescia P, Pedone C, Ianaro A, Cirino G
* Apolipoprotein A-I (ApoA-I) mimetic peptide P2a by restoring cholesterol esterification unmasks ApoA-I anti-inflammatory endogenous activity in vivo (335 visite)
J Pharmacol Exp Ther (ISSN: 1521-0103, 0022-3565), 2012 Mar; 340(3): 716-722.
Impact Factor: 3.891
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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 (338 visite)
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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Messalli G, Imbriaco M, Avitabile G, Russo R, Iodice D, Spinelli L, Dellegrottaglie S, Cademartiri F, Salvatore M, Pisani A
* Role of cardiac MRI in evaluating patients with Anderson-Fabry disease: Assessing cardiac effects of long-term enzyme replacement therapy (291 visite)
Radiol Med (ISSN: 0033-8362, 1826-6983, 1826-6983electronic), 2012 Feb; 117(1): 19-28.
Impact Factor: 1.461
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Langlois C, Del Gatto A, Arseneault G, Lafrance-vanasse J, De Simone M, Morse T, De Paola I, Lussier-price M, Legault P, Pedone C, Zaccaro L, Omichinski JG
* Structure-based design of a potent artificial transactivation domain based on p53 (380 visite)
J Am Chem Soc (ISSN: 1520-5126, 0002-2786, 0002-7863), 2012 Jan 25; 134(3): 1715-1723.
Impact Factor: 5.65
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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 (410 visite)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2012; 55(15): 6776-6783.
Impact Factor: 5.614
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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 (320 visite)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2012; 48(70): 8838-8840.
Impact Factor: 6.378
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Castellano I, Merlino A
* γ-glutamyltranspeptidases: Sequence, structure, biochemical properties, and biotechnological applications (363 visite)
Cell Mol Life Sci (ISSN: 1420-682x), 2012; 69(20): 3381-3394.
Impact Factor: 5.615
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Diana D, Basile A, De Rosa L, Di Stasi R, Auriemma S, Arra C, Pedone C, Turco MC, Fattorusso R, D'Andrea LD
* Beta-Hairpin Peptide That Targets Vascular Endothelial Growth Factor (vegf) Receptors: Design, Nmr Characterization, And Biological Activity (516 visite)
Jbc Papers (ISSN: 1083-351x, 0021-9258, 0021-9258linking), 2011 Dec 2; 286(48): 41680-41691.
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Scognamiglio PL, Doti N, Grieco P, Pedone C, Ruvo M, Marasco D
* Discovery Of Small Peptide Antagonists Of Ped/Pea15-D4alpha Interaction From Simplified Combinatorial Libraries (431 visite)
Chem Biol Drug Des Chemical Biology And Drug Design (ISSN: 1747-0277, 1747-0285), 2011 May; 77(5): 319-327.
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Basile A, Del Gatto A, Diana D, Di Stasi R, Falco A, Festa M, Rosati A, Barbieri A, Franco R, Arra C, Pedone C, Fattorusso R, Turco MC, D'Andrea LD
* Characterization of a designed vascular endothelial growth factor receptor antagonist helical peptide with antiangiogenic activity in vivo (425 visite)
J Med Chem (ISSN: 1520-4804, 0022-2623, 0022-2623print), 2011 Mar 10; 54(5): 1391-1400.
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Accardo A, Morisco A, Gianolio E, Tesauro D, Mangiapia G, Radulescu A, Brandt A, Morelli G
* Nanoparticles containing octreotide peptides and gadolinium complexes for MRI applications (456 visite)
J Pept Sci (ISSN: 1075-2617, 1099-1387, 1075-2617print), 2011 Feb; 17(2): 154-162.
Impact Factor: 1.799
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Milardi D, Sciacca MFM, Pappalardo M, Grasso DM, La Rosa C
* The Role Of Aromatic Side-Chains In Amyloid Growth And Membrane Interaction Of The Islet Amyloid Polypeptide Fragment Lanflvh (373 visite)
Eur Biophys J, 2011 Jan; 40(1): 1-12.
Impact Factor: 3.832
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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 (317 visite)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2011; 47(42): 11636-11638.
Impact Factor: 6.169
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Castellano I, Di Salle A, Merlino A, Rossi M, La Cara F
* Gene cloning and protein expression of γ-glutamyltranspeptidases from Thermus thermophilus and Deinococcus radiodurans: Comparison of molecular and structural properties with mesophilic counterparts (285 visite)
Extremophiles (ISSN: 1431-0651, 1433-4909, 1433-4909electronic), 2011; 15(2): 259-270.
Impact Factor: 2.941
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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 (299 visite)
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 (365 visite)
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, 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 (313 visite)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2010 Jun 15; 20(12): 3601-3605.
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Pensato S, Renda M, Leccia F, Saviano M, D'Andrea LD, Pedone C, Pedone PV, Romanelli A
* PNA zipper as a dimerization tool: development of a bZip mimic (446 visite)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 2010 May; 93(5): 434-441.
Impact Factor: 2.572
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Bruni AC, Bernardi L, Colao R, Rubino E, Smirne N, Frangipane F, Terni B, Curcio SA, Mirabelli M, Clodomiro A, Di Lorenzo R, Maletta R, Anfossi M, Gallo M, Geracitano S, Tomaino C, Muraca MG, Leotta A, Lio SG, Pinessi L, Rainero I, Sorbi S, Nee L, Milan G, Pappata S, Postiglione A, Abbamondi N, Forloni G, St George Hyslop P, Rogaeva E, Bugiani O, Giaccone G, Foncin JF, Spillantini MG, Puccio G
* Worldwide distribution of PSEN1 Met146Leu mutation: A large variability for a founder mutation (506 visite)
Neurology (ISSN: 0028-3878, 1526-632x, 1526-632xelectronic), 2010 Mar 9; 74(10): 798-806.
Impact Factor: 8.017
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De Simone G, Supuran CT
* Carbonic anhydrase IX: Biochemical and crystallographic characterization of a novel antitumor target (357 visite)
Bba-Gen Subjects (ISSN: 1570-9639, 0006-3002, 0925-4439), 2010 Feb; 1804(2): 404-409.
Impact Factor: 2.773
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Sciacca MFM, Pappalardo M, Attanasio F, Milardi D, La Rosa C, Grasso DM
* Are fibril growth and membrane damage linked processes? An experimental and computational study of IAPP(12-18) and IAPP(21-27) peptides (377 visite)
New J Chem (ISSN: 1144-0546), 2010; 34(2): 200-207.
Impact Factor: 2.631
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Guler OO, De Simone G, Supuran CT
* Drug design studies of the novel antitumor targets carbonic anhydrase IX and XII (437 visite)
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 (401 visite)
Curr Pharm Des Current Pharmaceutical Design (ISSN: 1381-6128, 1873-4286), 2010; 16(29): 3246-3254.
Impact Factor: 4.774
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Merlino A, Russo Krauss I, Perillo M, Mattia CA, Ercole C, Picone D, Vergara A, Sica F
* Toward an Antitumor Form of Bovine Pancreatic Ribonuclease: The Crystal Structure of Three Noncovalent Dimeric Mutants (361 visite)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 2009 Dec; 91(12): 1029-1037.
Impact Factor: 2.605
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Farina AR, Tacconelli A, Cappabianca L, Cea G, Chioda A, Romanelli A, Pensato S, Pedone C, Gulino A, Mackay AR
* The neuroblastoma tumour-suppressor TrkAI and its oncogenic alternative TrkAIII splice variant exhibit geldanamycin-sensitive interactions with Hsp90 in human neuroblastoma cells (344 visite)
Oncogene (ISSN: 1476-5594, 0950-9232), 2009 Nov 19; 28(46): 4075-4094.
Impact Factor: 7.135
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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 (393 visite)
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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De Simone G, Scozzafava A, Supuran CT
* Which Carbonic Anhydrases are Targeted by the Antiepileptic Sulfonamides and Sulfamates? (304 visite)
Chem Biol Drug Des Chemical Biology And Drug Design (ISSN: 1747-0277, 1747-0285), 2009 Sep; 74(3): 317-321.
Impact Factor: 2.473
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Imbriaco M, Pisani A, Spinelli L, Cuocolo A, Messalli G, Capuano E, Marmo M, Liuzzi R, Visciano B, Cianciaruso B, Salvatore M
* Effects of enzyme-replacement therapy in patients with Anderson-Fabry disease: a prospective long-term cardiac magnetic resonance imaging study (304 visite)
Heart (ISSN: 1355-6037, 1468-201x), 2009 Jul; 95(13): 1103-1107.
Impact Factor: 5.385
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De Rosa A, Criscuolo C, Mancini P, De Martino M, Giordano IA, Pappata S, Filla A, De Michele G
* Genetic screening for LRRK2 gene G2019S mutation in Parkinson's disease patients from Southern Italy (227 visite)
Parkinsonism Relat D (ISSN: 1353-8020print, 1353-8020linking, 1873-5126electronic), 2009 Mar; 15(3): 242-244.
Impact Factor: 2.406
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Kaczmarek K, Farina B, Zubrzak P, Jankowski S, Zimecki M, Suder P, Benedetti E, Fattorusso R, Saviano M, Zabrocki J
* Synthesis, conformational analysis and immunological activity of β3Phe-substituted Cyclolinopeptide A analogues (436 visite)
J Pept Sci (ISSN: 1075-2617, 1099-1387, 1075-2617print), 2009 Mar; 15(3): 166-174.
Impact Factor: 1.807
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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 (409 visite)
Proteins (ISSN: 1097-0134, 0887-3585, 1097-0134electronic), 2009 Jan; 74(1): 164-175.
Impact Factor: 3.085
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Merlino A, Avella G, Di Gaetano S, Arciello A, Piccoli R, Mazzarella L, Sica F
* Structural features for the mechanism of antitumor action of a dimeric human pancreatic ribonuclease variant (323 visite)
Protein Sci (ISSN: 0961-8368, 1469-896xelectronic, 0961-8368linking), 2009 Jan; 18(1): 50-57.
Impact Factor: 2.937
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Pentimalli F, Palmieri D, Pacelli R, Garbi C, Cesari R, Martin E, Pierantoni GM, Chieffi P, Croce CM, Costanzo V, Fedele M, Fusco A
* HMGA1 protein is a novel target of the ATM kinase (433 visite)
European Journal Of Cancer (ISSN: 0959-8049), 2008 Nov; 44(17): 2668-2679.
Impact Factor: 4.475
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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 (384 visite)
Jbc Papers (ISSN: 0021-9258, 1083-351x, 0021-9258linking), 2008 Oct 10; 283(41): 27799-27809.
Impact Factor: 5.52
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Dudar GK, D'Andrea LD, Di Stasi R, Pedone C, Wallace JL
* A vascular endothelial growth factor mimetic accelerates gastric ulcer healing in an iNOS-dependent manner (635 visite)
Am J Physiol Gastrointest Liver Physiol American Journal Of Physiology Gastrointestinal And Liver Physiology (ISSN: 0193-1857), 2008 Sep; 295(2): G374-G381.
Impact Factor: 3.587
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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 (443 visite)
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 (414 visite)
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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Esposito L, Paladino A, Pedone C, Vitagliano L
* Insights into structure, stability, and toxicity of monomeric and aggregated polyglutamine models from molecular dynamics simulations (315 visite)
Biophysical Journal (ISSN: 1542-0086, 0006-3495), 2008 May 15; 94(10): 4031-4040.
Impact Factor: 4.683
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Rendina D, De Filippo G, Viceconti R, Soscia E, Sirignano C, Salvatore M, Della Monica M, Scarano G, Mossetti G
* Interleukin (il)-6 And Receptor Activator Of Nuclear Factor (nf)-Kappab Ligand (rankl) Are Increased In The Serum Of A Patient With Primary Pachydermoperiostosis (411 visite)
Scand J Rheumatol (ISSN: 0300-9742), 2008 May; 37(3): 225-229.
Impact Factor: 2.345
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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 (361 visite)
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 (339 visite)
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 (386 visite)
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? (361 visite)
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 (333 visite)
Chemmedchem (ISSN: 1860-7179, 1860-7187, 1860-7187electronic), 2008 Mar; 3(3): 473-477.
Impact Factor: 3.15
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Merlino A, Ercole C, Picone D, Pizzo E, Mazzarella L, Sica F
* The buried diversity of bovine seminal ribonuclease: Shape and cytotoxicity of the swapped non-covalent form of the enzyme (350 visite)
J Mol Biol (ISSN: 0022-2836, 1089-8638, 1089-8638electronic), 2008 Feb 15; 376(2): 427-437.
Impact Factor: 4.146
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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 (332 visite)
Curr Pharm Des Current Pharmaceutical Design (ISSN: 1381-6128, 1873-4286), 2008; 14(7): 672-678.
Impact Factor: 4.399
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Giordano D, Vergara A, Lee HC, Peisach J, Balestrieri M, Mazzarella L, Parisi E, Di Priseo G, Verde C
* Hemoglobin structure/function and globin-gene evolution in the Arctic fish Liparis tunicatus (331 visite)
Gene (ISSN: 0378-1119), 2007 Dec 30; 406(1-2): 58-68.
Impact Factor: 2.871
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Calabrese V, Mancuso C, Calvani M, Rizzarelli E, Butterfield DA, Stella AM
* Nitric oxide in the central nervous system: neuroprotection versus neurotoxicity (494 visite)
Nature Reviews Neuroscience (ISSN: 1471-0048), 2007 Oct; 8(10): 766-775.
Impact Factor: 24.52
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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 (304 visite)
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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De Rosa A, Carducci C, Antonozzi I, Giovanniello T, Xhoxhi E, Criscuolo C, Menchise V, Striano S, Filla A, De Michele G
* A novel mutation in GCH-1 gene in a case of dopa-responsive dystonia [9] (288 visite)
J Neurol (ISSN: 0340-5354, 1432-1459, 1432-1459electronic), 2007 Sep; 254(8): 1133-1134.
Impact Factor: 2.477
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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 (311 visite)
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 (389 visite)
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 (396 visite)
Curr Top Med Chem (ISSN: 1568-0266, 1568-0266linking, 1873-4294electronic), 2007; 7(9): 879-884.
Impact Factor: 4.325
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Cucinotta V, Giuffrida A, Grasso G, Maccarrone G, Messina M, Vecchio G
* High selectivity in new chiral separations of dansyl amino acids by cyclodextrin derivatives in electrokinetic chromatography (260 visite)
J Chromatogr A (ISSN: 0021-9673), 2007; 1155(2): 172-179.
Impact Factor: 3.641
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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 (799 visite)
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 (280 visite)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2006 Dec 15; 16(24): 6204-6208.
Impact Factor: 2.538
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Pailot A, D'Ambrosio K, Corbier C, Talfournier F, Branlant G
* Invariant Thr(244) is essential for the efficient acylation step of the non-phosphorylating glyceraldehyde-3-phosphate dehydrogenase from Streptococcus mutans (301 visite)
Biochem J (ISSN: 0264-6021, 1470-8728electronic, 0264-6021linking), 2006 Dec 15; 400: 521-530.
Impact Factor: 4.1
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Saporito A, Marasco D, Chambery A, Botti P, Monti SM, Pedone C, Ruvo M
* The chemical synthesis of the GstI protein by NCL on a X-Met site (584 visite)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 2006 Dec 5; 83(5): 508-518.
Impact Factor: 2.48
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Dalla Bona A, Formaggio F, Peggion C, Kaptein B, Broxterman Quirinus B, Galdiero S, Galdiero M, Vitiello M, Benedetti E, Toniolo C
* Synthesis, conformation, and bioactivity of novel analogues of the antiviral lipopeptide halovir (427 visite)
J Pept Sci (ISSN: 1075-2617, 1099-1387, 1075-2617print), 2006 Dec; 12(12): 748-757.
Impact Factor: 1.801
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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 (417 visite)
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 (374 visite)
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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Merlino A, Esposito L, Vitagliano L
* Polyglutamine Repeats And Beta-Helix Structure: Molecular Dynamics Study (466 visite)
Proteins (ISSN: 0887-3585, 1097-0134, 1097-0134electronic), 2006 Jun 1; 63(4): 918-927.
Impact Factor: 3.73
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Mazzarella L, Bonomi G, Lubrano MC, Merlino A, Riccio A, Vergara A, Vitagliano L, Verde C, Di Prisco G
* Minimal structural requirements for root effect: Crystal structure of the cathodic hemoglobin isolated from the Antarctic fish Trematomus newnesi (447 visite)
Proteins (ISSN: 0887-3585, 1097-0134, 1097-0134electronic), 2006 Feb 1; 62(2): 316-321.
Impact Factor: 3.73
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D'Andrea LD, Del Gatto A, Pedone C, Benedetti E
* Peptide-based molecules in angiogenesis (612 visite)
Chem Biol Drug Des (ISSN: 1747-0277, 1747-0285, 1747-0277linking), 2006 Feb; 67(2): 115-126.
Impact Factor: 2.507
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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 (292 visite)
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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Iaccarino G, Izzo R, Trimarco V, Cipolletta E, Lanni F, Sorriento D, Iovino GL, Rozza F, De Luca N, Priante O, Di Renzo G, Trimarco B
* β 2-Adrenergic receptor polymorphisms and treatment-induced regression of left ventricular hypertrophy in hypertension (337 visite)
Clin Pharmacol Ther Clinical Pharmacology And Therapeutics (ISSN: 0009-9236), 2006; 80(6): 633-645.
Impact Factor: 8.066
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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 (306 visite)
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 (436 visite)
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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Esposito G, Vitagliano L, Cevenini A, Amelio T, Zagari A, Salvatore F
* Unraveling the structural and functional features of an aldolase A mutant involved in the hemolytic anemia and severe rhabdomyolysis reported in a child (311 visite)
Haematologica (ISSN: 0006-4971, 0006-6497, 0390-6078), 2005 Jan 15; 105(2): 905-906.
Impact Factor: 10.131
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Zubrzak P, Banas A, Kaczmarek K, Leplawy MT, Sochacki M, Kowalski ML, Szkudlinska B, Zabrocki J, Di Lello P, Isernia C, Saviano M, Pedone C, Benedetti E
* Analogues of cyclolinopeptide A containing alpha-hydroxymethyl amino acid residues (423 visite)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 2005; 80(2-3): 347-356.
Impact Factor: 2.425
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Merlino A, Graziano G, Mazzarella L
* Structural And Dynamic Effects Of Alpha-Helix Deletion In Sso7d: Implications For Protein Thermal Stability (325 visite)
Proteins (ISSN: 0887-3585, 1097-0134, 1097-0134electronic), 2004 Dec 1; 57(4): 692-701.
Impact Factor: 4.429
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Borgatti M, Finotti A, Romanelli A, Saviano M, Bianchi N, Lampronti I, Lambertini E, Penolazzi L, Nastruzzi C, Mischiati C, Piva R, Pedone C, Gambari R
* Peptide nucleic acids (PNA)-DNA chimeras targeting transcription factors as a tool to modify gene expression (452 visite)
Curr Drug Targets (ISSN: 1389-4501), 2004 Nov; 5(8): 735-744.
Impact Factor: 4.104
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Bonomo RP, Castronovo BM, Santoro AM
* A Spectroscopic Investigation Of The Interaction Between Nitrogen Monoxide And Copper Sites Of The Fungal Laccase From Rigidoporus Lignosus (260 visite)
Dalton Trans, 2004 Jan 7; N/D: 104-112.
Impact Factor: 4.097
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Russo M, Palumbo R, Mupo A, Tosto M, Iacomino G, Scognamiglio A, Tedesco I, Galano G, Russo GL
* Flavonoid quercetin sensitizes a CD95-resistant cell line to apoptosis by activating protein kinase Cα (334 visite)
Oncogene (ISSN: 0950-9232, 1476-5594), 2003; 22(21): 3330-3342.
Impact Factor: 6.495
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Orru S, Ruoppolo M, Francese S, Vitagliano L, Marino G, Esposito C
* Identification of tissue transglutaminase-reactive lysine residues in glyceraldehyde-3-phosphate dehydrogenase (9741 visite)
Protein Sci (ISSN: 0961-8368, 1469-896xelectronic), 2002 Jan; 11(1): 137-146.
Impact Factor: 3.546
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Garzillo AM, Colao MC, Buonocore V, Oliva R, Falcigno L, Saviano M, Santoro AM, Zappala R, Bonomo RP, Bianco C, Giardina P, Palmieri G, Sannia G
* Structural and kinetic characterization of native laccases from Pleurotas ostreatus, Rigidoporus lignosus, and Trametes trogii (347 visite)
Journal Of Protein Chemistry (ISSN: 0277-8033), 2001 Apr; 20(3): 191-201.
Impact Factor: 1.021
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Romanelli A, Garella I, Menchise V, Iacovino R, Saviano M, Montesarchio D, Didierjean C, Lello PD, Rossi F, Benedetti E
* Crystal-state conformation of Cα, α-dialkylated peptides containing chiral β-homo-residues (399 visite)
J Pept Sci (ISSN: 1075-2617, 1099-1387, 1075-2617print), 2001; 7(1): 15-26.
Impact Factor: 1.451
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De Simone G, Galdiero S, Manco G, Lang D, Rossi M, Pedone C
A snapshot of a transition state analogue of a novel thermophilic esterase belonging to the subfamily of mammalian hormone-sensitive lipase (400 visite)
J Mol Biol (ISSN: 0022-2836, 1089-8638, 1089-8638electronic), 2000 Nov 10; 303(5): 761-771.
Impact Factor: 5.388
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Esposito L, Vitagliano L, Sica F, Sorrentino G, Zagari A, Mazzarella L
The ultrahigh resolution crystal structure of ribonuclease A containing an isoaspartyl residue: Hydration and sterochemical analysis (389 visite)
J Mol Biol (ISSN: 0022-2836, 1089-8638, 1089-8638electronic), 2000 Mar 31; 297(3): 713-732.
Impact Factor: 5.388
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Oliva R, Falcigno L, D'Auria G, Zanotti G, Paolillo L
Conformation and calcium-binding properties of a bicyclic nonapeptide (326 visite)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 2000; 56(1): 27-36.
Impact Factor: 2.405
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Bonomo RP, Boudet AM, Cozzolino R, Rizzarelli E, Santoro AM, Sterjiades R, Zappalà R
A comparative study of two isoforms of laccase secreted by the 'white- rot' fungus Rigidoporus lignosus, exhibiting significant structural and functional differences (274 visite)
J Chem Res (ISSN: 0162-0134, 1873-3344, 0162-0134print), 1998 Sep; 71(3-4): 205-211.
Impact Factor: 1.162
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Arena G, Conato C, Contino A, Pulidori F, Purrello R, Remelli M, Tabbì G
Cu(II)-L-glutamine and L-asparagine binary complexes. A thermodynamic and spectroscopic study (277 visite)
Ann Chim (ISSN: 0003-4592), 1998 Jan; 88(1-2): 1-12.
Impact Factor: 0.811
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Benedetti E, Iacovino R, Pedone C, Rossi F, Saviano M, Isernia C, Montesarchio D, DeNapoli L, Piccialli G
β-Amino acid residues: Conformational characterization of an N- and C-protected homo-β-(S)-leucine (273 visite)
Int J Pept Res Ther (ISSN: 0929-5666, 1573-3149), 1997 Jun; 4(3): 129-134.
Impact Factor: 0.557
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Brunetti A, Alfano B, Soricelli A, Tedeschi E, Mainolfi C, Covelli EM, Aloj L, Panico M, Bazzicalupo L, Salvatore M
Functional characterization of brain tumors: An overview of the potential clinical value (477 visite) (PDF 227 visite)
Nucl Med Biol (ISSN: 0969-8051, 0883-2897), 1996 Sep; 23(6): 699-715.
Impact Factor: 1.042
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Pacelli R, Wink DA, Cook JA, Krishna MC, DeGraff W, Friedman N, Tsokos M, Samuni A, Mitchell JB
NITRIC-OXIDE POTENTIATES HYDROGEN PEROXIDE-INDUCED KILLING OF ESCHERICHIA-COLI (409 visite)
Journal Of Experimental Medicine (ISSN: 0022-1007), 1995 Nov 1; 182(5): 1469-1479.
Impact Factor: 14.384
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Di Blasio B, Saviano M, Del Duca V, De Simone G, Rossi F, Pedone C, Benedetti E, Lorenzi GP
CONFORMATIONAL STUDIES OF HETEROCHIRAL PEPTIDES WITH DIASTEREOISOMERIC RESIDUES - CRYSTAL AND MOLECULAR-STRUCTURES OF LINEAR DIPEPTIDES DERIVED FROM LEUCINE, ISOLEUCINE, AND ALLO-ISOLEUCINE (380 visite)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1995 Oct; 36(4): 401-408.
Impact Factor: 2.425
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Di Blasio B, Pavone V, Nastri F, Isernia C, Saviano M, Pedone C, Cucinotta V, Impellizzeri G, Rizzarelli E, Vecchio G
Conformation for a β-cyclodextrin monosubstituted with a cyclic dipeptide (430 visite)
P Natl Acad Sci Usa (ISSN: 0027-8424, 1091-6490, 0027-8424print), 1992 Sep 1; 89(15): 7218-7221.
Impact Factor: 9.04
Dettagli Esporta in BibTeX Esporta in EndNote
116 Records (114 escludendo Abstract e Conferenze).
Impact factor totale: 515.781 (507.132 escludendo Abstract e Conferenze).
Impact factor a 5 anni totale: 525.419 (515.9 escludendo Abstract e Conferenze).
Impact factor totale: 515.781 (507.132 escludendo Abstract e Conferenze).
Impact factor a 5 anni totale: 525.419 (515.9 escludendo Abstract e Conferenze).
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