期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 31, 期 6, 页码 1248-1253出版社
TAYLOR & FRANCIS LTD
DOI: 10.3109/14756366.2015.1120723
关键词
Acetate; alcohol; carbonic anhydrase; enzyme inhibition; enzyme purification; hydroperoxide
资金
- Research Chairs Program at King Saud University
The carbonic anhydrases (CAs, EC 4.2.1.1) represent a superfamily of widespread enzymes, which catalyze a crucial biochemical reaction, the reversible hydration of carbon dioxide to bicarbonate and protons. Human CA isoenzymes I and II (hCA I and hCA II) are ubiquitous cytosolic isoforms. In this study, a series of hydroperoxides, alcohols, and acetates were tested for the inhibition of the cytosolic hCA I and II isoenzymes. These compounds inhibited both hCA isozymes in the low nanomolar ranges. These compounds were good hCA I inhibitors (K(i)s in the range of 24.93-97.99 nM) and hCA II inhibitors (K(i)s in the range of 26.04-68.56 nM) compared to acetazolamide as CA inhibitor (K-i: 34.50nM for hCA I and K-i: 28.93nM for hCA II).
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