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首页> 外文期刊>Biochemistry >Role of the 20-hydroxyl group in camptothecin binding by the topoisomerase I-DNA binary complex.
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Role of the 20-hydroxyl group in camptothecin binding by the topoisomerase I-DNA binary complex.

机译：20-羟基在喜树碱中被拓扑异构酶I-DNA二元复合物结合的作用。

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摘要

Recent findings concerning the structure of the covalent binary complex formed by DNA topisomerase I and its DNA substrate, as well as the nature of interactions with inhibitors that bind reversibly to this binary complex, have led to two proposed models for the binding of the prototype inhibitor camptothecin to the DNA-topisomerase I binary complex. While these models differ in many regards, they both suggest the involvement of the 20-OH group of camptothecin in a donor hydrogen bond with an enzyme side chain functional group. Presently, five analogues of camptothecin that differ only at C-20 have been evaluated for their ability to bind to the topoisomerase I-DNA binary complex and thereby inhibit enzyme function. Both 20-chloro- and 20-bromocamptothecin bound as well to the enzyme-DNA binary complex as 20-aminoCPT despite the absence of a substituent at C-20 capable of contributing a donor hydrogen bond.
机译：有关由DNA拓扑异构酶I及其DNA底物形成的共价二元复合物的结构的最新发现，以及与可逆地结合至该二元复合物的抑制剂相互作用的性质，导致了两个提出的原型抑制剂结合模型喜树碱与DNA拓扑异构酶I的二元复合物。尽管这些模型在许多方面有所不同，但它们都表明喜树碱的20-OH基团与供体氢键和酶侧链官能团有关。目前，已经评价了喜树碱的仅在C-20处不同的五个类似物结合拓扑异构酶I-DNA二元复合物从而抑制酶功能的能力。尽管20-氯喜树碱和20-溴喜树碱与20-氨基CPT一样也与酶-DNA二元复合物结合，尽管在C-20处没有能够形成供体氢键的取代基。

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