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Carbonic anhydrase inhibitors: inhibition of the cytosolic human isozyme VII with anions.

Bioorganic & medicinal chemistry letters (2006-04-20)
Daniela Vullo, Eva Ruusuvuori, Kai Kaila, Andrea Scozzafava, Claudiu T Supuran
RÉSUMÉ

An inhibition study of the cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isozyme VII (hCA VII) with anions has been conducted. Cyanate, cyanide, and hydrogensulfite were weak hCA VII inhibitors (K(I)s in the range of 7.3-15.2 mM). Cl- and HCO3- showed good inhibitory activity against hCA VII (K(I)s of 0.16-1.84 mM), suggesting that this enzyme is not involved in metabolons with anion exchangers or sodium bicarbonate cotransporters. The best inhibitors were sulfamate, sulfamide, phenylboronic, and phenylarsonic acid (K(I)s of 6.8-12.5 microM).

MATÉRIAUX
Référence du produit
Marque
Description du produit

Sigma-Aldrich
Acide sulfurique, ACS reagent, 95.0-98.0%
Sigma-Aldrich
Acide sulfurique, 99.999%
Sigma-Aldrich
Phenylboronic acid, 95%
Supelco
Acide sulfurique solution, 0.1 M H2SO4 in water (0.2N), eluent concentrate for IC
Supelco
Acide sulfurique, for the determination of nitrogen, ≥97.0%
Sigma-Aldrich
Sulfamide, 99%
Sigma-Aldrich
Acide sulfurique, puriss., meets analytical specification of Ph. Eur., BP, 95-97%