Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 21, Issue 15, Pages 4521-4525Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.05.042
Keywords
Carbonic anhydrase; Anion; alpha-Class enzyme; Inhibitor; Sulfurihydrogenibium azorense; Thermophilic bacteria
Funding
- FP7 EU Project (Metoxia)
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The alpha-carbonic anhydrase (CA, EC 4.2.1.1) from the newly discovered extremophilic bacterium Sulfurihydrogenibium azorense (SazCA) is the most effective CA known to date. Here we investigated the inhibition profile of this enzyme with a series of aromatic and heterocyclic sulfonamides, and one sulfamate. Many clinically used sulfonamides, such as acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, topiramate, celecoxib and sulpiride were low nanomolar/subnanomolar SazCA inhibitors (K(I)s in the range of 0.9-10.8 nM) whereas simple aromatic derivatives were less effective as SazCA inhibitors. The inhibition profile of SazCA is slightly different from that of the related enzyme from S. yellostonense (SspCA), investigated earlier by our groups. (C) 2013 Elsevier Ltd. All rights reserved.
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