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Biochemistry. 1989 May 2;28(9):3886-94.

Mechanism of inhibition of DNA gyrase by quinolone antibacterials: a cooperative drug--DNA binding model.

Author information

1
Anti-Infective Research Division, Abbott Laboratories, Abbott Park, Illinois 60064.

Abstract

We have proposed a cooperative quinolone-DNA binding model for the inhibition of DNA gyrase. The essential feature of the model is that bound gyrase induces a specific quinolone binding site in the relaxed DNA substrate in the presence of ATP. The binding affinity and specificity are derived from two unique and equally important functional features: the specific conformation of the proposed single-stranded DNA pocket induced by the enzyme and the unique self-association phenomenon (from which the cooperativity is derived) of the drug molecules to fit the binding pocket with a high degree of flexibility. Supporting evidence for and implications of this model are provided.

PMID:
2546585
DOI:
10.1021/bi00435a039
[Indexed for MEDLINE]

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