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

Proceedings of the National Academy of Sciences of the United States of America
Thota GaneshD G Kingston

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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Citations

Apr 1, 2014·Bioorganic & Medicinal Chemistry·Iwao OjimaJacob G Vineberg
Jan 11, 2007·Journal of the American Chemical Society·Younkee PaikDavid G I Kingston
Nov 4, 2008·The Journal of Organic Chemistry·Liang SunIwao Ojima
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Jan 3, 2008·Physical Chemistry Chemical Physics : PCCP·Elizabeth M HeiderDavid M Grant
Nov 29, 2008·Organic & Biomolecular Chemistry·Qiao-Hong ChenDavid G I Kingston
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