Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides

Bertucci, Anthony, Innocenti, Alessio, Zoccola, Didier, Scozzafava, Andrea, Tambutté, Sylvie, and Supuran, Claudiu T. (2009) Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides. Bioorganic & Medicinal Chemistry, 17 (14). pp. 5054-5058.

[img] PDF (Published Version) - Published Version
Restricted to Repository staff only

View at Publisher Website: http://dx.doi.org/10.1016/j.bmc.2009.05....
 
30
4


Abstract

The inhibition of a newly cloned coral carbonic anhydrase (CA, EC 4.2.1.1) has been investigated with a series of sulfonamides, including some clinically used derivatives (acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, benzolamide, and sulpiride, or indisulam, a compound in clinical development as antitumor drug), as well as the sulfamate antiepileptic topiramate. Some simple amino-/hydrazine-/hydroxy-substituted aromatic/heterocyclic sulfonamides have also been included in the study. All types of activity have been detected, with low potency inhibitors (KIs in the range of 163–770 nM), or with medium potency inhibitors (KIs in the range of 75.1–105 nM), whereas ethoxzolamide, several clinically used sulfonamides and heterocyclic compounds showed stronger potency, with KIs in the range of 16–48.2 nM. These inhibitors may be useful to better understand the physiological role of the Stylophora pistillata CA (STPCA) in corals and its involvement in biomineralisation in this era of global warming.

Item ID: 31633
Item Type: Article (Research - C1)
ISSN: 1464-3391
Keywords: carbonic anhydrase; scleractinian corals; biomineralisation; sulfonamide; enzyme inhibitor; secreted enzyme
Funders: European Union Sixth Framework Program (EU FP6), Fund for Investment in Basic Research (FIRB), Government of the Principality of Monaco
Projects and Grants: EU FP6 DeZnIT project, FIRB MIUR/FIRB RBNE03PX83_001
Date Deposited: 16 Oct 2014 01:35
FoR Codes: 06 BIOLOGICAL SCIENCES > 0601 Biochemistry and Cell Biology > 060107 Enzymes @ 50%
06 BIOLOGICAL SCIENCES > 0606 Physiology > 060604 Comparative Physiology @ 50%
SEO Codes: 97 EXPANDING KNOWLEDGE > 970106 Expanding Knowledge in the Biological Sciences @ 100%
Downloads: Total: 4
More Statistics

Actions (Repository Staff Only)

Item Control Page Item Control Page