Carbonic anhydrase inhibitors: inhibition studies of a coral secretory isoform with inorganic anions

Bioorg Med Chem Lett. 2009 Feb 1;19(3):650-3. doi: 10.1016/j.bmcl.2008.12.056. Epub 2008 Dec 24.

Abstract

The inhibition of a coral carbonic anhydrase (CA, EC 4.2.1.1) has been investigated with a series of inorganic anions such as halogenides, pseudohalogenides, bicarbonate, carbonate, nitrate, nitrite, hydrogen sulfide, bisulfite, perchlorate, sulfate. The full-length scleractinian coral Stylophora pistillata CA, STPCA, has a significant catalytic activity for the physiological reaction of CO(2) hydration to bicarbonate, similarly to the ubiquitous human isoforms hCA I (cytosolic) and hCA VI (secreted). The best STPCA anion inhibitors were bromide, iodide, carbonate, and sulfamate, with inhibition constants of 9.0-10.0 microM.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetazolamide / chemistry
  • Amino Acid Sequence
  • Animals
  • Anions / chemistry
  • Anthozoa
  • Binding Sites
  • Carbon Dioxide / chemistry
  • Carbonic Anhydrase Inhibitors / chemical synthesis*
  • Carbonic Anhydrase Inhibitors / chemistry*
  • Carbonic Anhydrases / chemistry*
  • Drug Design*
  • Humans
  • Isoenzymes / chemistry
  • Kinetics
  • Molecular Sequence Data
  • Protein Isoforms
  • Sequence Homology, Amino Acid

Substances

  • Anions
  • Carbonic Anhydrase Inhibitors
  • Isoenzymes
  • Protein Isoforms
  • Carbon Dioxide
  • Carbonic Anhydrases
  • Acetazolamide