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紫杉烷结合、溶液中蛋白结合构象及紫杉烷类及其衍生物的抗有丝分裂细胞特性分析。

Tubulin binding, protein-bound conformation in solution, and antimitotic cellular profiling of noscapine and its derivatives.

机构信息

Vertex Pharmaceuticals Inc., 130 Waverly Street, Cambridge Massachusetts 02139, USA.

出版信息

J Med Chem. 2012 Mar 8;55(5):1920-5. doi: 10.1021/jm200848t. Epub 2012 Feb 27.

Abstract

Noscapine and its 7-hydroxy and 7-amino derivatives were characterized for their binding to tubulin. A solution NMR structure of these compounds bound to tubulin shows that noscapine and its 7-aniline derivative do not compete for the same binding site nor does its small molecule crystal structure match its tubulin-bound conformation. These compounds were also tested for their antiproliferative effects on a panel hepatocellular carcinoma cell lines.

摘要

纳库巴因及其 7-羟基和 7-氨基衍生物的结合特性进行了研究。这些化合物与微管蛋白结合的溶液 NMR 结构表明,纳库巴因及其 7-苯胺衍生物不竞争相同的结合位点,其小分子晶体结构也与其微管蛋白结合构象不匹配。这些化合物还在一组肝癌细胞系中进行了抗增殖作用测试。

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