The bioactive Taxol conformation on β-tubulin:: Experimental evidence from highly active constrained analogs

被引：98

作者：

Ganesh, T

Guza, RC

Bane, S

Ravindra, R

Shanker, N

Lakdawala, AS

Snyder, JP

Kingston, DGI

机构：

[1] Virginia Polytech Inst & State Univ, Dept Chem, Blacksburg, VA 24061 USA

[2] Emory Univ, Dept Chem, Atlanta, GA 30322 USA

[3] SUNY Binghamton, Dept Chem, Binghamton, NY 13902 USA

来源：

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA | 2004年 / 101卷 / 27期

关键词：

D O I：

10.1073/pnas.0403459101

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

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.

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页码：10006 / 10011

页数：6

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