title: Mode of action of GR122222X, a novel inhibitor of bacterial DNA gyrase.
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.
authors.affiliation: Department of Cellular and Molecular Sciences, University of London, United Kingdom.
authors.forename: M
authors.initials: M
authors.lastname: Oram
authors.forename: B
authors.initials: B
authors.lastname: Dosanjh
authors.forename: N A
authors.initials: NA
authors.lastname: Gormley
authors.forename: C V
authors.initials: CV
authors.lastname: Smith
authors.forename: L M
authors.initials: LM
authors.lastname: Fisher
authors.forename: A
authors.initials: A
authors.lastname: Maxwell
authors.forename: K
authors.initials: K
authors.lastname: Duncan
mesh_terms: D004250:DNA Topoisomerases, Type II / Q000378:metabolism; D009675:Novobiocin / Q000378:metabolism / Q000494:pharmacology; D010456:Peptides, Cyclic / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D059005:Topoisomerase II Inhibitors
chemical_list: D010456:Peptides, Cyclic; D059005:Topoisomerase II Inhibitors; C088717:GR 122222X; D009675:Novobiocin; D004250:DNA Topoisomerases, Type II