• 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