The bioactive Taxol conformation on beta-tubulin: experimental evidence from highly active constrained analogs.

Ganesh, Thota; Guza, Rebecca C; Bane, Susan; Ravindra, Rudravajhala; Shanker, Natasha; Lakdawala, Ami S; Snyder, James P; Kingston, David G I · Proc Natl Acad Sci U S A · 2004

basic_science · Level V

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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.

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