β-微管蛋白上的生物活性紫杉醇构象：来自高活性受限类似物的实验证据。
The bioactive Taxol conformation on beta-tubulin: experimental evidence from highly active constrained analogs.
作者信息
Ganesh Thota, Guza Rebecca C, Bane Susan, Ravindra Rudravajhala, Shanker Natasha, Lakdawala Ami S, Snyder James P, Kingston David G I
机构信息
Department of Chemistry, M/C 0212, Virginia Polytechnic Institute and State University, Blacksburg, VA 24061, USA.
出版信息
Proc Natl Acad Sci U S A. 2004 Jul 6;101(27):10006-11. doi: 10.1073/pnas.0403459101. Epub 2004 Jun 28.
Abstract
The important anticancer drug Taxol (paclitaxel) binds to tubulin in a stoichiometric ratio and promotes its assembly into microtubules. The conformation of microtubule-bound drug has been the subject of intense study, and various suggestions have been made. In this work we present experimental and theoretical evidence that Taxol adopts a T-shaped conformation when it is bound to tubulin.
摘要
重要的抗癌药物紫杉醇（paclitaxel）以化学计量比与微管蛋白结合，并促进其组装成微管。与微管结合的药物的构象一直是深入研究的主题，并且已经提出了各种建议。在这项工作中，我们提供了实验和理论证据，表明紫杉醇与微管蛋白结合时呈T形构象。
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