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

Bioorg Med Chem Lett. 2006 Jun 15;16(12):3139-43. doi: 10.1016/j.bmcl.2006.03.078. Epub 2006 Apr 18.

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).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anions / chemistry
  • Carbonic Anhydrase Inhibitors / pharmacology*
  • Carbonic Anhydrases / metabolism*
  • Cytoplasm / drug effects*
  • Cytoplasm / enzymology*
  • Humans
  • Isoenzymes / metabolism
  • Mice

Substances

  • Anions
  • Carbonic Anhydrase Inhibitors
  • Isoenzymes
  • Carbonic Anhydrases