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Antimicrobial Agents and Chemotherapy, Feb 1996, 473-476, Vol 40, No. 2
Copyright © 1996 by the American Society for Microbiology. All rights reserved.

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

M Oram, B Dosanjh, NA Gormley, CV Smith, LM Fisher, A Maxwell and K Duncan
Department of Cellular and Molecular Sciences, University of London, United Kingdom.

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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