The structure of human recombinant aldose reductase complexed with the potent inhibitor zenarestat.

Kinoshita T; Miyake H; Fujii TTakakura SGoto T

首页> 外文期刊>Acta crystallographica.Section D. Biological crystallography >The structure of human recombinant aldose reductase complexed with the potent inhibitor zenarestat.

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The structure of human recombinant aldose reductase complexed with the potent inhibitor zenarestat.

机译：人类重组醛糖的结构还原酶复合体与强有力的抑制剂

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The crystal structure of the complex of human recombinant aldose reductase (AR) with zenarestat, one of its potent inhibitors, has been solved at 2.5 A resolution. Zenarestat fits neatly in the hydrophobic active site and induces unique and dramatic conformational changes. For example, the benzene ring of zenarestat occupies a gap in the side chains of Leu300 and Trp111 that interact directly and forms a CH-pi interaction in the native holoenzyme. As a result, the benzene ring of the inhibitor and these side chains form a CH-pi-pi interaction. Such structural information is key to understanding the mode of action of this class of inhibitors and for rational design of better therapeutics.

机译：人类的复杂的晶体结构重组醛糖还原酶(AR)它的一个强有力的抑制剂,zenarestat解决了在2.5一项决议。整齐的疏水活性部位和诱导独特和引人注目的构象变化。例子,zenarestat占据的苯环侧链的差距Leu300和Trp111直接交互,形成CH-pi本机全酶相互作用。结果,苯环的抑制剂这些侧链形成CH-pi-pi交互。这样的结构信息是关键了解这类行动的模式抑制剂和更好的合理的设计疗法。

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来源
《Acta crystallographica.Section D. Biological crystallography》 |2002年第4期|622-626|共5页
作者
Kinoshita T; Miyake H; Fujii TTakakura SGoto T;
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作者单位

Exploratory Research Laboratories, Fujisawa Pharmaceutical Co. Ltd, 5-2-3, Tokodai, Tsukuba, Ibaraki 300-2698, Japan. takayoshi_kinoshita@po.fujisawa.co.jp;

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正文语种英语
中图分类化学;
关键词
Aldehyde Reductase; crystal structure; FR 74366quinazolineEnzyme InhibitorsAlcohol Dehydrogenase;

机译：醛还原酶;晶体结构;FR74366 quinazolineenzyme InhibitorsAlcohol脱氢酶;

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The structure of human recombinant aldose reductase complexed with the potent inhibitor zenarestat.

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