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The interaction between coumarin drugs and DNA gyrase
Author(s) -
Maxwell Anthony
Publication year - 1993
Publication title -
molecular microbiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.857
H-Index - 247
eISSN - 1365-2958
pISSN - 0950-382X
DOI - 10.1111/j.1365-2958.1993.tb01728.x
Subject(s) - dna gyrase , dna supercoil , biology , coumarin , dna , enzyme , biochemistry , novobiocin , topoisomerase , protein subunit , atpase , antibiotics , escherichia coli , gene , dna replication , botany
Summary The 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.