The interaction between coumarin drugs and DNA gyrase

Molecular Microbiology - Tập 9 Số 4 - Trang 681-686 - 1993
Anthony Maxwell1
1Department of Biochemistry University of Leicester, Leicester LE1 7RH, UK

Tóm tắt

SummaryThe coumarin group of antibiotics have as their target the bacterial enzyme DNA gyrase. The drugs bind to the B subunit of gyrase and inhibit DNA supercoiling by blocking the ATPase activity. Recent data show that the binding site for the drugs lies within the N‐terminal part of the B protein, and individual amino acids involved in coumarin interaction are being identified. The mode of inhibition of the gyrase ATPase reaction by coumarins is unlikely to be simple competitive inhibition, and the drugs may act by stabilizing a conformation of the enzyme with low affinity for ATP.

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