Title of article
Carbonic anhydrase inhibitors: The β-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors
Author/Authors
Isao Nishimori، نويسنده , , Tomoko Minakuchi، نويسنده , , Takuhiro Kohsaki، نويسنده , , Saburo Onishi، نويسنده , , Hiroaki Takeuchi، نويسنده , , Daniela Vullo، نويسنده , , Andrea Scozzafava، نويسنده , , Claudiu T. Supuran، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
10
From page
3585
To page
3594
Abstract
DNA clones for the β-class carbonic anhydrase (CA, EC 4.2.1.1) of Helicobactor pylori (hpβCA) were obtained. A recombinant hpβCA protein lacking the N-terminal 15-amino acid residues was produced and purified, representing a catalytically efficient CA. hpβCA was strongly inhibited (KIs 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 α- and/or β-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 β-CA can be a drug target.
Keywords
Catalytic/inhibition mechanism , carbonic anhydrase , Helicobacter pylori , ?-class enzyme , Sulfonamide , Enzyme inhibitor , Sulfamate
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798276
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