Lewis R J, Tsai F T, Wigley D B
Laboratory of Molecular Biophysics, University of Oxford, UK.
Bioessays. 1996 Aug;18(8):661-71. doi: 10.1002/bies.950180810.
DNA gyrase, an enzyme unique to prokaryotes, has been implicated in almost all processes that involve DNA. Although efficient inhibitors of this protein have been known for more than 20 years, none of them have enjoyed prolonged pharmaceutical success. It is only recently that the mechanisms of inhibition for some of these classes of drugs have been established unequivocally by X-ray crystallography. It is hoped that this detailed structural information will assist the design of novel, effective inhibitors of DNA gyrase.
DNA 促旋酶是原核生物特有的一种酶，几乎参与了所有涉及 DNA 的过程。尽管这种蛋白质的有效抑制剂已被发现二十多年，但它们都未在制药领域取得长期成功。直到最近，通过 X 射线晶体学才明确确定了其中一些药物的抑制机制。人们希望这些详细的结构信息将有助于设计新型、有效的 DNA 促旋酶抑制剂。
