期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 13, 页码 3585-3594出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.04.063
关键词
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DNA clones for the P-class carbonic anhydrase (CA, EC 4.2.1.1) of Helicobactor pylori (hp beta CA) were obtained. A recombinant hp beta CA protein lacking the N-terminal 15-arnino acid residues was produced and purified, representing a catalytically efficient CA. hp beta CA was strongly inhibited (K(1)s in the range of 24-45 nM) by many sulfonamides/sulfamates, among which acetazolamide, ethoxzolamide, topiramate, and sulpiride, all clinically used drugs. The dual inhibition of alpha- and/or beta-class CAs of H. pylori might represent a useful alternative for the management of gastritis/gastric ulcers, as well as gastric cancer. This is also the first study showing that a bacterial beta-CA can be a drug target. (c) 2007 Elsevier Ltd. All rights reserved.
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