期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 5, 页码 1548-1550出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.01.081
关键词
Carbonic anhydrase; Transmembrane isoforms; CA IX; CA XII; CA XIV; Trithiocarbonate; Dialkyldithiocarbamates
资金
- European Union
An inhibition study of the transmembrane carbonic anhydrase (CA, EC 4.2.1.1) isoforms IX, XII (tumor-associated), and XIV with anions such as stannate(IV), selenate(VI), tellurate(VI), perosmate(VIII), persulfate, pyrophosphate(V), pyrovanadate(V), tetraborate, persulfate, perrhenate(VII), perrutenate(VII), selenocyanate, iminodisulfonate, fluorosulfate, and trithiocarbonate is reported. Selenate, perosmate, and pyrophosphate were ineffective inhibitors, whereas most of these anions inhibited the three enzymes in the millimolar-submillimolar range. Trithiocarbonate and diethyldithiocarbamate were the best CA IX inhibitors (K(I)s of 1.4-9.7 mu M), but trithiocarbonate showed less affinity for CA XII and XIV (K(I)s of 0.12-0.66 mM). N,N-Diethyldithiocarbamate was a low micromolar inhibitor also against CA XII and XIV (KIs of 1.0-1.1 mu M), suggesting that this new zinc-binding group (CS2-) may lead to efficient inhibitors targeting transmembrane CAs. (C) 2010 Elsevier Ltd. All rights reserved.
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