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

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
ABSTRACT

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).

MATERIALS
Product Number
Brand
Product Description

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