| Literature DB >> 17482815 |
Isao Nishimori1, Tomoko Minakuchi, Takuhiro Kohsaki, Saburo Onishi, Hiroaki Takeuchi, Daniela Vullo, Andrea Scozzafava, Claudiu T Supuran.
Abstract
DNA clones for the beta-class carbonic anhydrase (CA, EC 4.2.1.1) of Helicobactor pylori (hpbetaCA) were obtained. A recombinant hpbetaCA protein lacking the N-terminal 15-amino acid residues was produced and purified, representing a catalytically efficient CA. hpbetaCA was strongly inhibited (K(I)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.Entities:
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Year: 2007 PMID: 17482815 DOI: 10.1016/j.bmcl.2007.04.063
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823