2. Academic Validation
  3. Mode of action of GR122222X, a novel inhibitor of bacterial DNA gyrase

Mode of action of GR122222X, a novel inhibitor of bacterial DNA gyrase

  • Antimicrob Agents Chemother. 1996 Feb;40(2):473-6. doi: 10.1128/AAC.40.2.473.
M Oram 1,  B Dosanjh,  N A Gormley,  C V Smith,  L M Fisher,  A Maxwell,  K Duncan
Affiliations

Affiliation

  • 1 Department of Cellular and Molecular Sciences, University of London, United Kingdom.
PMID: 8834902 DOI: 10.1128/AAC.40.2.473
Abstract

GR122222X is a potent inhibitor of the supercoiling reaction of Bacterial DNA gyrase. We show that this compound binds stoichiometrically to inactivate the ATPase activity of a 43-kDa N-terminal fragment of the B subunit and competitively inhibits the binding of a radiolabelled coumarin drug to N-terminal fragments of GyrB. These and other data suggest that GR122222X has a mode of action similar, but not identical, to that of coumarin Antibiotics.

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