Maxwell A
Department of Biochemistry, University of Leicester, UK.
Mol Microbiol. 1993 Aug;9(4):681-6. doi: 10.1111/j.1365-2958.1993.tb01728.x.
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.
香豆素类抗生素的作用靶点是细菌酶DNA旋转酶。这些药物与旋转酶的B亚基结合，并通过阻断ATP酶活性来抑制DNA超螺旋化。最近的数据表明，药物的结合位点位于B蛋白的N端部分，并且参与香豆素相互作用的个别氨基酸正在被确定。香豆素对旋转酶ATP酶反应的抑制模式不太可能是简单的竞争性抑制，这些药物可能通过稳定对ATP亲和力低的酶构象来发挥作用。
