Carbonic anhydrase activators: Activation of human isozymes I,II and IX with phenylsulfonylhydrazido l-histidine derivatives |
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| Authors: | Marie-Rose Abdo Daniela Vullo Mohamed-Chiheb Saada Jean-Louis Montero Andrea Scozzafava Jean-Yves Winum Claudiu T Supuran |
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| Institution: | 1. Institut des Biomolécules Max Mousseron (IBMM) UMR 5247 CNRS-UM1-UM2 Bâtiment de Recherche Max Mousseron, Ecole Nationale Supérieure de Chimie de Montpellier, 8 rue de l’Ecole Normale, 34296 Montpellier Cedex, France;2. Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy |
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| Abstract: | Activation of the human carbonic anhydrase (CA, EC 4.2.1.1) isozymes I, II (cytosolic) and IX (transmembrane, tumor-associated isoform) with a series of arylsulfonylhydrazido-l-histidines incorporating 4-substituted-phenyl, pentafluorophenyl- and β-naphthyl moieties was investigated. The compounds showed a weak hCA I activation profile, but were more efficient as hCA II and IX activators. The 4-iodophenyl-substituted derivative behaved as a strong and isozyme selective hCA II activator, with an activation constant of 0.21 μM. This is the first isoform-selective, potent CA activator reported to date. |
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