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Benzoxaborole as a new chemotype for carbonic anhydrase inhibition (78 visite)

Alterio V, Cadoni R, Esposito D, Vullo D, Fiore AD, Monti SM, Caporale A, Ruvo M, Sechi M, Dumy P, Supuran CT, De Simone G, Winum JY

Chem Commun (ISSN: 1364-548xelectronic, 1359-7345linking), 2016 Sep 29; 52(80): 11983-11986.

Tipo di articolo: Journal Article,

Impact factor: 6.319

Impact factor a 5 anni: 6.238


Parole chiave: Non disponibili.

Url: http://pubs.rsc.org/en/content/articlelanding/2016/cc/c6cc06399c#!divRelatedContent

In this paper we report the synthesis of a series of benzoxaborole derivatives, their inhibition properties against some carbonic anhydrases (CAs), recognized as important drug targets, and the characterization of the binding mode of these molecules to the CA active site. Our data provide the first experimental evidence that benzoxaboroles can be efficiently used as CA inhibitors.
*** IBB - CNR ***

Istituto di Biostrutture e Bioimagini-CNR, Naples, Italy. 
  • Institut des Biomolécules Max Mousseron (IBMM) UMR5247 CNRS, ENSCM, Université de Montpellier, Montpellier, France.
  • Laboratorio di Chimica Bioinorganica, Polo Scientifico, Università degli Studi di Firenze, Sesto Fiorentino, Florence, Italy.
  • Dipartimento di Chimica e Farmacia, Università degli Studi di Sassari, Sassari, Italy.
  • Neurofarba Department, Section of Pharmaceutical and Nutriceutical Sciences, Università degli Studi di Firenze, Sesto Fiorentino, Florence, Italy.
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    Contiene: [X]      Estesa  

    Autori: [X]   E Tipo di lavoro: [X]

    E Data iniziale: Data finale: [X]   E Sede:  E    Affiliazione IBB  
        
    [Pulisci modulo]
    Alterio V, Esposito D, Monti SM, Supuran CT, De Simone G
    * Crystal structure of the human carbonic anhydrase II adduct with 1-(4-sulfamoylphenyl-ethyl)-2, 4, 6-triphenylpyridinium perchlorate, a membrane-impermeant, isoform selective inhibitor (214 visite)
    J Enzyme Inhib Med Chem (ISSN: 1475-6374electronic, 1475-6366linking), 2018 Dec; 33(1): 151-157.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    Monti SM, Meccariello A, Ceruso M, Szafranski K, Slawinski J, Supuran CT
    * Inhibition studies of Brucella suis beta-carbonic anhydrases with a series of 4-substituted pyridine-3-sulphonamides (67 visite)
    J Enzyme Inhib Med Chem (ISSN: 1475-6374electronic, 1475-6366linking), 2018 Dec; 33(1): 255-259.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    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 (15 visite)
    Chem Commun (ISSN: 1364-548xelectronic, 1359-7345linking), 2018 Sep 11; 54(73): 10312-10315.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    Langella E, Buonanno M, Vullo D, Dathan N, Leone M, Supuran C, De Simone G, Monti SM
    * Biochemical, biophysical and molecular dynamics studies on the proteoglycan-like domain of carbonic anhydrase IX (28 visite)
    Cell Mol Life Sci, 2018 Sep; 75: 3283-3296.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    Supuran CT, Alterio V, Di Fiore A, D'Ambrosio K, Carta F, Monti SM, De Simone G
    * Inhibition of carbonic anhydrase IX targets primary tumors, metastases, and cancer stem cells: Three for the price of one (18 visite)
    Med Res Rev (ISSN: 1098-1128electronic, 0198-6325linking), 2018 Sep; 38(6): 1799-1836.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    Di Fiore A, Monti DM, Scaloni A, De Simone G, Monti SM
    * Protective Role of Carbonic Anhydrases III and VII in Cellular Defense Mechanisms upon Redox Unbalance (23 visite)
    Oxid Med Cell Longev, 2018 Aug; 2018:2018306: N/D-N/D.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    Ferrucci V, De Antonellis P, Pennino FP, Asadzadeh F, Virgilio A, Montanaro D, Galeone A, Boffa I, Pisano I, Scognamiglio I, Navas L, Diana D, Pedone E, Gargiulo S, Gramanzini M, Brunetti A, Danielson L, Carotenuto M, Liguori L, Verrico A, Quaglietta L, Errico ME, Del Monaco V, D'Argenio V, Tirone F, Mastronuzzi A, Donofrio V, Giangaspero F, Picard D, Remke M, Garzia L, Daniels C, Delattre O, Swartling FJ, Weiss WA, Salvatore F, Fattorusso R, Chesler L, Taylor MD, Cinalli G, Zollo M
    * Metastatic group 3 medulloblastoma is driven by PRUNE1 targeting NME1-TGF-beta-OTX2-SNAIL via PTEN inhibition (69 visite)
    (ISSN: 1460-2156electronic, 0006-8950linking), 2018 Feb 27; N/D: N/D-N/D.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    Monti DM, De Simone G, Langella E, Supuran CT, Di Fiore A, Monti SM
    * Insights into the role of reactive sulfhydryl groups of Carbonic Anhydrase III and VII during oxidative damage (99 visite)
    J Enzyme Inhib Med Chem (ISSN: 1475-6374electronic, 1475-6366linking), 2017 Dec; 32(1): 5-12.
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    Camorani S, Hill BS, Fontanella R, Greco A, Gramanzini M, Auletta L, Gargiulo S, Albanese S, Lucarelli E, Cerchia L, Zannetti A
    * Inhibition of Bone Marrow-Derived Mesenchymal Stem Cells Homing Towards Triple-Negative Breast Cancer Microenvironment Using an Anti-PDGFRbeta Aptamer (302 visite) (PDF 89 visite)
    Theranostics (ISSN: 1838-7640electronic, 1838-7640linking), 2017 Aug 22; 7(14): 3595-3607.
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    Tomasello MF, Nardon C, Lanza V, Di Natale G, Pettenuzzo N, Salmaso S, Milardi D, Caliceti P, Pappalardo G, Fregona D
    * New comprehensive studies of a gold(III) Dithiocarbamate complex with proven anticancer properties: Aqueous dissolution with cyclodextrins, pharmacokinetics and upstream inhibition of the ubiquitin-proteasome pathway (79 visite)
    Eur J Med Chem (ISSN: 1768-3254electronic, 0223-5234linking), 2017 Jun 19; 138: 115-127.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    Sciacca MFM, Romanucci V, Zarrelli A, Monaco I, Lolicato F, Spinella N, Galati C, Grasso G, D'Urso L, Romeo M, Diomede L, Salmona M, Bongiorno C, Di Fabio G, La Rosa C, Milardi D
    * Inhibition of Abeta Amyloid Growth and Toxicity by Silybins: The Crucial Role of Stereochemistry (75 visite) (PDF 82 visite)
    Acs Chem Neurosci (ISSN: 1948-7193electronic, 1948-7193linking), 2017 Jun 09; N/D: N/D-N/D.
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    Pirone L, Ripoll-rozada J, Leone M, Ronca R, Lombardo F, Fiorentino G, Andersen JF, Pereira PJB, Arcà B, Pedone E
    * Functional analyses yield detailedinsight into the mechanism of thrombin inhibition by the antihemostatic salivary protein cE5 from Anopheles gambiae (48 visite) (PDF 72 visite)
    Jbc Papers, 2017 Jun; N/D: N/D-N/D.
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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 (88 visite)
    J Med Chem, 2017 May 25; 60: 4316-4326.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    Buonanno M, Langella E, Zambrano N, Succoio M, Sasso E, Alterio V, Di Fiore A, Sandomenico A, Supuran CT, Scaloni A, Monti SM, De Simone G
    * Disclosing the Interaction of Carbonic Anhydrase IX with Cullin-Associated NEDD8-Dissociated Protein 1 by Molecular Modeling and Integrated Binding Measurements (74 visite)
    Acs Chem Biol (ISSN: 1554-8937electronic, 1554-8929linking), 2017 Apr 19; N/D: N/D-N/D.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    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 (60 visite)
    J Med Chem (ISSN: 1520-4804electronic, 0022-2623linking, 0022-2623print), 2017 Mar 23; 60(6): 2456-2469.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    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 (58 visite)
    Bioorg Med Chem (ISSN: 1464-3391electronic, 0968-0896linking), 2017 Feb 15; 25(4): 1456-1464.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    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 (64 visite)
    Bioorg Med Chem (ISSN: 1464-3391electronic, 0968-0896linking), 2017 Jan 15; pii:S0968-0896(16): 539-544.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    Palumbo R, Gogliettino M, Cocca E, Iannitti R, Sandomenico A, Ruvo M, Balestrieri M, Rossi M, Palmieri G
    * APEH Inhibition Affects Osteosarcoma Cell Viability via Downregulation of the Proteasome (74 visite)
    Int J Mol Sc (ISSN: 1422-0067electronic, 1422-0067linking, 1661-6596), 2016 Sep 23; 17(10): N/D-N/D.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    Vullo D, Supuran CT, Scozzafava A, De Simone G, Monti SM, Alterio V, Carta F
    * Kinetic and X-ray crystallographic investigations of substituted 2-thio-6-oxo-1, 6-dihydropyrimidine-benzenesulfonamides acting as carbonic anhydrase inhibitors (63 visite)
    Bioorg Med Chem (ISSN: 1464-3391electronic, 0968-0896linking), 2016 Aug 15; 24(16): 3643-3648.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    Pelagalli A, Nardelli A, Fontanella R, Zannetti A
    * Inhibition of AQP1 Hampers Osteosarcoma and Hepatocellular Carcinoma Progression Mediated by Bone Marrow-Derived Mesenchymal Stem Cells (103 visite) (PDF 193 visite)
    Int J Mol Sc (ISSN: 1422-0067electronic, 1422-0067linking, 1661-6596), 2016 Jul 11; 17(7): N/D-N/D.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    Di Fiore A, De Simone G, Alterio V, Riccio V, Winum JY, Carta F, Supuran CT
    * The anticonvulsant sulfamide JNJ-26990990 and its S, S-dioxide analog strongly inhibit carbonic anhydrases: solution and X-ray crystallographic studies (83 visite)
    Org Biomol Chem (ISSN: 1477-0520linking, 1477-0539electronic), 2016 Jun 07; 14(21): 4853-4858.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    Del Prete S, De Luca V, De Simone G, Supuran CT, Capasso C
    * Cloning, expression and purification of the complete domain of the eta-carbonic anhydrase from Plasmodium falciparum (77 visite)
    J Enzyme Inhib Med Chem (ISSN: 1475-6374electronic, 1475-6366linking), 2016 Jun; 31(sup4): 54-59.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    Langella E, D'Ambrosio K, D'Ascenzio M, Carradori S, Monti SM, Supuran CT, De Simone G
    * A Combined Crystallographic and Theoretical Study Explains the Capability of Carboxylic Acids to Adopt Multiple Binding Modes in the Active Site of Carbonic Anhydrases (101 visite)
    Chemistry (ISSN: 1521-3765electronic, 0947-6539linking), 2016 Jan 4; 22(1): 97-100.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    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 (75 visite)
    J Enzyme Inhib Med Chem, 2016; 17: 1-6.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    Mollica A, Locatelli M, Macedonio G, Carradori S, Sobolev AP, De Salvador RF, Monti SM, Buonanno M, Zengin G, Angeli A, Supuran CT
    * Microwave-assisted extraction, HPLC analysis, and inhibitory effects on carbonic anhydrase I, II, VA, and VII isoforms of 14 blueberry Italian cultivars (65 visite)
    J Enzyme Inhib Med Chem, 2016; 31(sup4): N/D-N/D.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    De Rosa V, Iommelli F, Monti M, Fonti R, Votta G, Stoppelli MP, Del Vecchio S
    * Reversal of Warburg Effect and Reactivation of Oxidative Phosphorylation by Differential Inhibition of EGFR Signaling Pathways in Non-Small Cell Lung Cancer (304 visite)
    Clin Cancer Res (ISSN: 1078-0432linking, 1078-0432electronic, 1078-0432print), 2015 Nov 15; 21(22): 5110-5120.
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    La Regina G, Coluccia A, Famiglini V, Pelliccia S, Monti L, Vullo D, Nuti E, Alterio V, De Simone G, Monti SM, Pan P, Parkkila S, Supuran CT, Rossello A, Silvestri R
    * Discovery of 1, 1'-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors (121 visite)
    J Med Chem (ISSN: 1520-4804electronic, 0022-2623linking, 0022-2623print), 2015 Nov 12; 58(21): 8564-8572.
    Dettagli    Esporta in BibTeX    Esporta in EndNote

    Di Fiore A, Vergara A, Caterino M, Alterio V, Monti SM, Ombouma J, Dumy P, Vullo D, Supuran CT, Winum JY, De Simone G
    * Hydroxylamine-O-sulfonamide is a versatile lead compound for the development of carbonic anhydrase inhibitors (136 visite) (PDF 125 visite)
    Chem Commun (ISSN: 1364-548xelectronic, 1359-7345linking), 2015 Jul 2; 51(57): 11519-11522.
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    De Simone G, Monti SM, Alterio V, Buonanno M, De Luca V, Rossi M, Carginale V, Supuran CT, Capasso C, Di Fiore A
    * Crystal structure of the most catalytically effective carbonic anhydrase enzyme known, SazCA from the thermophilic bacterium Sulfurihydrogenibium azorense (97 visite)
    Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2015 May 1; 25(9): 2002-2006.
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    Alterio V, Tanc M, Ivanova J, Zalubovskis R, Vozny I, Monti SM, Di Fiore A, De Simone G, Supuran CT
    * X-ray crystallographic and kinetic investigations of 6-sulfamoyl-saccharin as a carbonic anhydrase inhibitor (139 visite)
    Org Biomol Chem (ISSN: 1477-0539electronic, 1477-0520linking), 2015 Apr 7; 13(13): 4064-4069.
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    De Simone G, Di Fiore A, Capasso C, Supuran CT
    * The zinc coordination pattern in the eta-carbonic anhydrase from Plasmodium falciparum is different from all other carbonic anhydrase genetic families (224 visite)
    Bioorg Med Chem Lett (ISSN: 1464-3405electronic, 0960-894xlinking), 2015 Apr 1; 25(7): 1385-1389.
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    Alterio V, Langella E, De Simone G, Monti SM
    * Cadmium-containing carbonic anhydrase CDCA1 in marine diatom Thalassiosira weissflogii (145 visite)
    Marine Drugs (ISSN: 1660-3397electronic, 1660-3397linking), 2015 Apr; 13(4): 1688-1697.
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    Supuran CT, Capasso C, De Simone G
    * Carbonic Anhydrase II as Target for Drug Design (85 visite)
    Carbonic Anhydrases As Biocatalysts, 2015 Jan 08; N/D: 51-90.
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    Monti SM, Supuran CT, De Simone G, Di Fiore A
    * Carbonic Anhydrase VII (72 visite)
    Carbonic Anhydrases As Biocatalysts, 2015 Jan 08; N/D: 151-168.
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    Supuran CT, De Simone G
    Carbonic Anhydrases: An Overview (79 visite)
    Carbonic Anhydrases As Biocatalysts, 2015 Jan 08; N/D: 3-13.
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    D'Ambrosio K, De Simone G, Supuran CT
    * Human Carbonic Anhydrases: Catalytic Properties, Structural Features, and Tissue Distribution (83 visite)
    Carbonic Anhydrases As Biocatalysts, 2015 Jan 08; N/D: 17-30.
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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 (147 visite) (PDF 125 visite)
    Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2015 Jan 7; 51(2): 302-305.
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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 (110 visite)
    Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 1464-3391electronic), 2015; 23(15): 4181-4187.
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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 (105 visite)
    Biomed Res Int (ISSN: 2314-6133, 2314-6141, 2314-6141electronic), 2015; 2015: 174178-174178.
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    Di Fiore A, Alterio V, Monti SM, De Simone G, D’Ambrosio K
    * Thermostable carbonic anhydrases in biotechnological applications (117 visite)
    Int J Mol Sc (ISSN: 1661-6596, 1422-0067, 1422-0067electronic), 2015; 16(7): 15456-15480.
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    Doti N, Reuther C, Scognamiglio PL, Dolga AM, Plesnila N, Ruvo M, Culmsee C
    * Inhibition of the AIF/CypA complex protects against intrinsic death pathways induced by oxidative stress (125 visite)
    Cell Death Dis (ISSN: 2041-4889, 2041-4889electronic), 2014 Jan 16; 5(1): e993-e993.
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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" (118 visite)
    J Enzyme Inhib Med Chem (ISSN: 1475-6366, 1475-6374electronic, 1475-6366linking), 2014; 29(4): 500-504.
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    De Simone G, Pizika G, Monti SM, Di Fiore A, Ivanova J, Vozny I, Trapencieris P, Zalubovskis R, Supuran CT, Alterio V
    * Hydrophobic substituents of the phenylmethylsulfamide moiety can be used for the development of new selective carbonic anhydrase inhibitors (105 visite)
    Biomed Res Int (ISSN: 2314-6133, 2314-6141, 2314-6141electronic), 2014; 2014: 523210-523210.
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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 (123 visite)
    Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 2014; 101(7): 769-778.
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    Alterio V, Monti SM, De Simone G
    * Thermal-stable carbonic anhydrases: a structural overview (146 visite)
    Subcell Biochem (ISSN: 0306-0225), 2014; 75: 387-404.
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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 (161 visite)
    J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2013 Nov 14; 56(21): 8512-8520.
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    De Rosa V, Iommelli F, Votta G, Monti M, Ortosecco G, Fonti R, Mainolfi C, Stoppelli M, Del Vecchio S
    * Changes of Glycolytic Pathway in Response to Efficient Inhibition of EGFR Signaling in Non-small Cell Lung Cancer (NSCLC) (83 visite)
    Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2013 Oct; 40: N/D-N/D.
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    De Simone G, Alterio V, Supuran CT
    * Exploiting the hydrophobic and hydrophilic binding sites for designing carbonic anhydrase inhibitors (134 visite)
    Expert Opin Drug Discov (ISSN: 1746-0441), 2013 Jul; 8(7): 793-810.
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    Monti SM, Supuran CT, De Simone G
    * Anticancer carbonic anhydrase inhibitors: A patent review (2008-2013) (131 visite)
    Expert Opin Ther Pat Expert Opinion On Therapeutic Patents (ISSN: 1354-3776), 2013 Jun; 23(6): 737-749.
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    Di Fiore A, Capasso C, De Luca V, Monti SM, Carginale V, Supuran CT, Scozzafava A, Pedone C, Rossi M, De Simone G
    * X-ray structure of the first 'extremo-alpha-carbonic anhydrase', a dimeric enzyme from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 (110 visite)
    Acta Crystallogr D Biol Crystallogr (ISSN: 0907-4449, 0907-4449linking), 2013 Jun; 69(6): 1150-1159.
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    Monti SM, De Simone G, Dathan NA, Ludwig M, Vullo D, Scozzafava A, Capasso C, Supuran CT
    * Kinetic And Anion Inhibition Studies Of A Beta-Carbonic Anhydrase (fbica 1) From The C-4 Plant Flaveria Bidentis (121 visite)
    Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2013 Mar 15; 23(6): 1626-1630.
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    Buanne P, Renzone G, Monteleone F, Vitale M, Monti SM, Sandomenico A, Garbi C, Montanaro D, Accardo M, Troncone G, Zatovicova M, Csaderova L, Supuran CT, Pastorekova S, Scaloni A, De Simone G, Zambrano N
    * Characterization of carbonic anhydrase ix interactome reveals proteins assisting its nuclear localization in hypoxic cells (109 visite)
    J Proteome Res Journal Of Proteome Research (ISSN: 1535-3893), 2013 Jan; 12(1): 282-292.
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    Del Giudice R, Monti DM, Truppo E, Arciello A, Supuran CT, De Simone G, Monti SM
    * Human Carbonic Anhydrase Vii Protects Cells From Oxidative Damage (112 visite)
    Biol Chem Biological Chemistry (ISSN: 1431-6730, 1431-1673, 1437-4315), 2013; 394(10): 1343-1348.
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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? (122 visite)
    Chemical Reviews (ISSN: 0009-2665), 2012 Sep; 112(8): 4421-4468.
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    De Simone G, Supuran CT
    * (In)organic anions as carbonic anhydrase inhibitors (119 visite)
    J Chem Res (ISSN: 0162-0134, 1873-3344, 0162-0134print), 2012 Jun; 111: 117-129.
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    Alterio V, Langella E, Viparelli F, Vullo D, Ascione G, Dathan NA, Morel FM, Supuran CT, De Simone G, Monti SM
    * Structural and inhibition insights into carbonic anhydrase CDCA1 from the marine diatom Thalassiosira weissflogii (130 visite)
    Biochimie (ISSN: 0300-9084, 1638-6183, 1638-6183electronic), 2012 May; 94(5): 1232-1241.
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    Sandomenico A, Russo A, Palmieri G, Bergamo P, Gogliettino M, Falcigno L, Ruvo M
    * Small peptide inhibitors of acetyl-peptide hydrolase having an uncommon mechanism of inhibition and a stable bent conformation (99 visite)
    J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2012 Mar 8; 55(5): 2102-2111.
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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 (90 visite)
    Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2012 Feb 15; 22(4): 1560-1564.
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    Monti SM, Supuran CT, De Simone G
    * Carbonic anhydrase IX as a target for designing novel anticancer drugs (163 visite)
    Curr Med Chem (ISSN: 0929-8673, 1875-533x, 1875-533xelectronic), 2012 Feb; 19(6): 821-830.
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    Monti SM, Maresca A, Viparelli F, Carta F, De Simone G, Muehlschlegel FA, Scozzafava A, Supuran CT
    * Dithiocarbamates are strong inhibitors of the beta-class fungal carbonic anhydrases from Cryptococcus neoformans, Candida albicans and Candida glabrata (108 visite)
    Bioorg Med Chem Lett (ISSN: 0960-894x), 2012 Jan 15; 22(2): 859-862.
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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 (117 visite)
    J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2012; 55(15): 6776-6783.
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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 (87 visite)
    Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2012; 48(70): 8838-8840.
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    Folgiero V, Di Carlo SE, Bossi G, Spugnini E, Di Benedetto A, Bon G, Milella M, Fabi A, Accardo A, Morelli G, Mottolese M, Falcioni R
    * Inhibition of p85, the non-catalytic subunit of phosphatidylinositol 3-kinase, exerts potent antitumor activity in human breast cancer cells (104 visite)
    Cell Death Dis (ISSN: 2041-4889, 2041-4889electronic), 2012; 3(12): N/D-N/D.
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    Palmieri G, Bergamo P, Luini A, Ruvo M, Gogliettino M, Langella E, Saviano M, Hegde RN, Sandomenico A, Rossi M
    * Acylpeptide Hydrolase Inhibition as Targeted Strategy to Induce Proteasomal Down-Regulation (125 visite)
    Plos One (ISSN: 1932-6203, 1932-6203electronic), 2011 Oct 10; 6(10): N/D-N/D.
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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 (95 visite)
    Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2011; 47(42): 11636-11638.
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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 (112 visite)
    Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2010 Sep 15; 20(16): 4745-4748.
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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 (115 visite)
    Org Biomol Chem (ISSN: 1477-0520, 1477-0539, 1477-0539electronic), 2010 Sep 7; 8(15): 3528-3533.
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    Pensato S, Saviano M, Bianchi N, Borgatti M, Fabbri E, Gambari R, Romanelli A
    * Gamma-Hydroxymethyl Pnas: Synthesis, Interaction With Dna And Inhibition Of Protein/Dna Interactions (100 visite)
    Bioorg Chem, 2010 Sep; 38(5): 196-201.
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    Palmieri C, Falcone C, Iaccino E, Tuccillo FM, Gaspari M, Trimboli F, De Laurentiis A, Luberto L, Pontoriero M, Pisano A, Vecchio E, Fierro O, Panico M, Larobina M, Gargiulo S, Costa N, Dal Piaz F, Schiavone M, Arra C, Giudice A,  Palma G, Barbieri A, Quinto I, Scala G
    * In vivo targeting and growth inhibition of the A20 murine B-cell lymphoma by an idiotype-specific peptide binder (127 visite)
    Haematologica (ISSN: 0006-4971, 0006-6497, 0390-6078), 2010 Jul 15; 116(2): 226-238.
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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 (91 visite)
    Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2010 Jun 15; 20(12): 3601-3605.
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    De Simone G, Supuran CT
    * Carbonic anhydrase IX: Biochemical and crystallographic characterization of a novel antitumor target (147 visite)
    Biochim Biophys Acta (ISSN: 1570-9639, 0006-3002, 0925-4439), 2010 Feb; 1804(2): 404-409.
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    Guler OO, De Simone G, Supuran CT
    * Drug design studies of the novel antitumor targets carbonic anhydrase IX and XII (191 visite)
    Curr Med Chem (ISSN: 0929-8673, 1875-533x, 1875-533xelectronic), 2010; 17(15): 1516-1526.
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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 (106 visite)
    Curr Pharm Des Current Pharmaceutical Design (ISSN: 1381-6128, 1873-4286), 2010; 16(29): 3246-3254.
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    Innocenti A, Pastorekova S, Pastorek J, Scozzafava A, De Simone G, Supuran CT
    * The proteoglycan region of the tumor-associated carbonic anhydrase isoform IX acts as anintrinsic buffer optimizing CO2 hydration at acidic pH values characteristic of solid tumors (73 visite)
    Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2009 Oct 15; 19(20): 5825-5828.
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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 (145 visite)
    J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2009 Oct 8; 52(19): 5990-5998.
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    Alterio V, Hilvo M, Di Fiore A, Supuran CT, Pan P, Parkkila S, Scaloni A, Pastorek J, Pastorekova S, Pedone C, Scozzafava A, Monti SM, De Simone G
    * Crystal structure of the catalytic domain of the tumor-associated human carbonic anhydrase IX (178 visite)
    Proc Natl Acad Sci U S A (ISSN: 0027-8424, 1091-6490, 0027-8424print), 2009 Sep 22; 106(38): 16233-16238.
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    De Simone G, Scozzafava A, Supuran CT
    * Which Carbonic Anhydrases are Targeted by the Antiepileptic Sulfonamides and Sulfamates? (96 visite)
    Chem Biol Drug Des Chemical Biology And Drug Design (ISSN: 1747-0277, 1747-0285), 2009 Sep; 74(3): 317-321.
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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 (92 visite)
    Proteins (ISSN: 1097-0134, 0887-3585, 1097-0134electronic), 2009 Jan; 74(1): 164-175.
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    Hilvo M, De Simone G, Supuran CT, Parkkila S
    * Advances in the Inhibitory and Structural Investigations on Carbonic Anhydrase Isozymes XIII and XV (99 visite)
    Drug Des Of Zinc Enzyme Inhibitors (ISSN: 9780-4702, 9780-470275009), 2009; N/D: 273-283.
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    De Simone G, Supuran CT
    * Drug Design of Antiobesity Carbonic Anhydrase Inhibitors (115 visite)
    Drug Des Of Zinc Enzyme Inhibitors (ISSN: 9780-4702, 9780-470275009), 2009; 66(DECEMBERSPEC.I): 241-254.
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    Alterio V, Di Fiore A, D'Ambrosio K, Supuran CT, De Simone G
    * X-Ray Crystallography of Carbonic Anhydrase Inhibitors and Its Importance in Drug Design (112 visite)
    Drug Des Of Zinc Enzyme Inhibitors (ISSN: 9780-4702, 9780-470275009), 2009; N/D: 73-138.
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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 (116 visite)
    J Biol Chem Journal Of Biological Chemistry (ISSN: 0021-9258, 1083-351x), 2008 Oct 10; 283(41): 27799-27809.
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    De Bona P, Giuffrida ML, Attanasio F, Copani A, Pignataro B, Cataldo S, Rizzarelli E, Pappalardo G
    * Designing trehalose-conjugated peptides for the inhibition of Alzheimer's A beta oligornerization and neurotoxicity (111 visite)
    J Pept Sci (ISSN: 1075-2617, 1099-1387, 1075-2617print), 2008 Sep; 14(8): N/D-N/D.
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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 (126 visite)
    J Med Chem (ISSN: 1520-4804, 0022-2623, 0022-2623print), 2008 Jun 12; 51(11): 3230-3237.
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    Supuran CT, Di Fiore A, De Simone G
    * Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity (122 visite)
    Expert Opin Emerg Drugsexpert Opinion On Emerging Drugs (ISSN: 1472-8214), 2008 Jun; 13(2): 383-392.
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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 (98 visite)
    Bioorg Med Chem Lett (ISSN: 1464-3405, 0960-894x, 1464-3405electronic), 2008 Apr 15; 18(8): 2669-2674.
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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 (73 visite)
    Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2008 Apr 1; 18(7): 2267-2271.
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    De Simone G, Di Fiore A, Supuran CT
    * Are carbonic anhydrase inhibitors suitable for obtaining antiobesity drugs? (111 visite)
    Curr Pharm Des Current Pharmaceutical Design (ISSN: 1381-6128, 1873-4286), 2008 Mar; 14(7): 655-660.
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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 (144 visite)
    Chemmedchem (ISSN: 1860-7179, 1860-7187, 1860-7187electronic), 2008 Mar; 3(3): 473-477.
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    Sabbatino F, Pacelli R, Punzo G, Fusciello C, Vernieri C, Della Vittoria Scarpati G, Pepe S
    * Inhibition of poly (ADP-Ribose) polymerase synergizes with the DNA-topoisomerase-1-inhibitor, topotecan, and radiation in human glioblastoma cell lines (79 visite)
    Cytometry Part A (ISSN: 1552-4922), 2008 Jan; 73A(1): N/D-N/D.
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    Supuran CT, De Simone G
    Carbonic anhydrases--an overview (104 visite)
    Curr Pharm Des, 2008; 14(7): 603-614.
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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 (101 visite)
    Curr Pharm Des Current Pharmaceutical Design (ISSN: 1381-6128, 1873-4286), 2008; 14(7): 672-678.
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    Malaguarnera R, Vella V, Pandini G, Sanfilippo M, Pezzino V, Vigneri R, Frasca F
    * TAp73α increases p53 tumor suppressor activity in thyroid cancer cells via the inhibition of Mdm2-mediated degradation (105 visite)
    Mol Cancer Res (ISSN: 1541-7786), 2008; 6(1): 64-77.
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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 (96 visite)
    Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2007 Sep 1; 17(15): 4201-4207.
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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 (107 visite)
    Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 1464-3391electronic), 2007 Jun 15; 15(12): 4152-4158.
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    Galdiero S, Falanga A, Vitiello M, D'Isanto M, Collins C, Orrei V, Browne H, Pedone C, Galdiero M
    * Evidence for a role of the membrane-proximal region of herpes simplex virus type 1 glycoprotein H in membrane fusion and virus inhibition (103 visite)
    Chembiochem (ISSN: 1439-4227, 1439-7633, 1439-7633electronic), 2007 May 25; 8(8): 885-895.
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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 (114 visite)
    Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2007 Mar 15; 17(6): 1726-1731.
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    De Simone G, Supuran CT
    * Antiobesity carbonic anhydrase inhibitors (145 visite)
    Curr Top Med Chem (ISSN: 1568-0266, 1568-0266linking, 1873-4294electronic), 2007; 7(9): 879-884.
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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 (99 visite)
    Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2006 Dec 15; 16(24): 6204-6208.
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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 (128 visite)
    J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2006 Sep 7; 49(18): 5544-5551.
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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 (108 visite)
    J Am Chem Soc (ISSN: 0002-7863, 0002-2786, 1520-5126), 2006 Jun 28; 128(25): 8329-8335.
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    Iommelli F, Zannetti A, Pepe S, Sabbatino F, Laus G, Ghidelli L, Solla R, Scala S, Del Vecchio S, Salvatore M, Pacelli R
    * Inhibition of NF-kappa B activity potentiates ionizing radiation and cisplatin induced cell killing of anaplastic thyroid carcinoma cells (95 visite)
    Meetingproceedings Of The American Association For Cancer Research Annual (ISSN: 0197-016x), 2006 Apr; 47: N/D-N/D.
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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 (105 visite)
    Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2006 Jan 15; 16(2): 437-442.
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    Zannetti A, Del Vecchio S, Romanelli A, Scala S, Saviano M, Cali' G, Stoppelli MP, Pedone C, Salvatore M
    * Inhibition of Sp1 activity by a decoy PNA-DNA chimera prevents urokinase receptor expression and migration of breast cancer cells (108 visite)
    Biochem Pharmacol Biochemical Pharmacology (ISSN: 0006-2952, 1873-2968), 2005 Nov 1; 70(9): 1277-1287.
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    Menchise V, De Simone G, Alterio V, Di Fiore A, Pedone C, Scozzafava A, Supuran CT
    * Carbonic anhydrase inhibitors: Stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide complexed with isozyme II (131 visite)
    J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2005 Sep 8; 48(18): 5721-5727.
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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 (106 visite)
    Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2005 May 2; 15(9): 2315-2320.
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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 (129 visite)
    Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2005 Apr 1; 15(7): 1937-1942.
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    La Rosa C, Milardi D, Amato E, Pappalardo M, Grasso D
    * Molecular mechanism of the inhibition of cytochrome c aggregation by Phe-Gly (127 visite)
    Arch Biochem Biophys (ISSN: 0003-9861), 2005 Mar 1; 435(1): 182-189.
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    Bashan A, Zarivach R, Schluenzen F, Agmon I, Harms J, Auerbach T, Baram D, Berisio R, Bartels H, Hansen HAS, Fucini P, Wilson D, Peretz M, Kessler M, Yonath A
    * Ribosomal crystallography: Peptide bond formation and its inhibition (107 visite)
    Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 2003 Sep; 70(1): 19-41.
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    Del Vecchio S, Zannetti A, Aloj L, Caracò C, Ciarmiello A, Salvatore M
    * Inhibition of early Tc-99m-MIBI uptake by Bcl-2 anti-apoptotic protein overexpression in untreated breast carcinoma (121 visite)
    Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2003 Jun; 30(6): 879-887.
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    Fonti R, Latella G, Caprilli R, Frieri G, Marcheggiano A, Sambuy Y
    Carbonic anhydrase I reduction in colonic mucosa of patients with active ulcerative colitis (70 visite)
    Digestive Diseases And Sciences (ISSN: 0163-2116), 1998; 43(9): 2086-2092.
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    Condorelli G, Costanzo LL, De Guidi G, Giuffrida S, Rizzarelli E, Vecchio G
    INHIBITION OF PHOTOHEMOLYSIS BY COPPER(II) COMPLEXES WITH SOD-LIKE ACTIVITY (111 visite)
    J Chem Res (ISSN: 0162-0134, 1873-3344, 0162-0134print), 1994 Jun; 54(4): 257-265.
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    112 Records (105 escludendo Abstract e Conferenze).
    Impact factor totale: 497.312 (472.032 escludendo Abstract e Conferenze).
    Impact factor a 5 anni totale: 477.971 (452.379 escludendo Abstract e Conferenze).







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