氟喹诺酮类药物的作用机制。

Mechanism of fluoroquinolone action.

作者信息

Drlica K

机构信息

Public Health Research Institute 455 First Avenue, New York, NY 10016, USA.

出版信息

Curr Opin Microbiol. 1999 Oct;2(5):504-8. doi: 10.1016/s1369-5274(99)00008-9.

DOI:10.1016/s1369-5274(99)00008-9

PMID:10508721

Abstract

When fluoroquinolones bind to gyrase or topoisomerase IV in the presence of DNA, they alter protein conformation. DNA cleavage results with diminished religation, so the enzymes are trapped in ternary complexes with drug and cleaved DNA. Preferential localization of gyrase ahead of replication forks and topoisomerase IV behind them causes fluoroquinolone-mediated complexes with the two enzymes to have different physiological consequences.

摘要

当氟喹诺酮类药物在有DNA存在的情况下与回旋酶或拓扑异构酶IV结合时，它们会改变蛋白质构象。DNA断裂导致再连接减少，因此这些酶被困在与药物和断裂DNA形成的三元复合物中。回旋酶在复制叉之前的优先定位以及拓扑异构酶IV在复制叉之后的优先定位，使得氟喹诺酮介导的与这两种酶形成的复合物产生不同的生理后果。