Structural basis for specificity and potency of a flavonoid inhibitor of human CDK2, a cell cycle kinase

Walter Filgueira de Azevedo Jr; Hans-Joachim Mueller-Dieckmann; Ursula Schulze-Gahmen

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Structural basis for specificity and potency of a flavonoid inhibitor of human CDK2, a cell cycle kinase

机译：人CDK2（一种细胞周期激酶）类黄酮抑制剂的特异性和效力的结构基础

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The central role of cyclin-dependent kinases (CDKs) in cell cycle regulation makes them a promising target for studying inhibitory molecules that can modify the degree of cell proliferation. The discovery of specific inhibitors of CDKs such as polyhydroxylated flavones has opened the way to inves- tigation and design of antimitotic compounds. A novel flavone, (-)-cis-5,7-dihydroxyphenyl-8-[4-(3-hydroxy-1-methyl)piperidi- nyl]-4H-1-benzopyran-4-one hydrochloride hemihydrate (L868276), is a potent inhibitor of CDKs.

机译：细胞周期蛋白依赖性激酶（CDKs）在细胞周期调控中的核心作用使它们成为研究可改变细胞增殖程度的抑制性分子的有希望的目标。 CDK特定抑制剂（例如多羟基黄酮）的发现为研究和设计抗有丝分裂化合物开辟了道路。一种新型黄酮（-）-顺5,7-二羟基苯基-8- [4-（3-羟基-1-甲基）哌啶基] -4H-1-苯并吡喃-4-酮盐酸盐半水合物（L868276），是CDK的有效抑制剂。

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《Proceedings of the National Academy of Sciences of the United States of America》 |1996年第7期|p.2735-2740|共6页
作者
Walter Filgueira de Azevedo Jr; Hans-Joachim Mueller-Dieckmann; Ursula Schulze-Gahmen;
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收录信息美国《科学引文索引》(SCI);美国《生物学医学文摘》(MEDLINE);美国《化学文摘》(CA);
原文格式 PDF
正文语种 eng
中图分类自然科学总论;
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6. Structural basis for specificity and potency of a flavonoid inhibitor of human CDK2 a cell cycle kinase. [O] . W F De Azevedo Jr, H J Mueller-Dieckmann, U Schulze-Gahmen, 1996

机译：人CDK2（一种细胞周期激酶）类黄酮抑制剂的特异性和效力的结构基础。
7. Structural basis for specificity and potency of a flavonoid inhibitor of human CDK2, a cell cycle kinase. [O] . De Azevedo, W F, Mueller-Dieckmann, H J, Schulze-Gahmen, U, 1996

机译：人CDK2（一种细胞周期激酶）类黄酮抑制剂的特异性和效力的结构基础。

Structural basis for specificity and potency of a flavonoid inhibitor of human CDK2, a cell cycle kinase

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