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

Thota Ganesh | Zendy; Rebecca Guza | Zendy; Susan Bane | Zendy; Rudravajhala Ravindra | Zendy; Natasha Shanker | Zendy; Ami S. Lakdawala | Zendy; James P. Snyder | Zendy; David G. I. Kingston | Zendy

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

Author(s) -

Thota Ganesh,

Rebecca Guza,

Susan Bane,

Rudravajhala Ravindra,

Natasha Shanker,

Ami S. Lakdawala,

James P. Snyder,

David G. I. Kingston

Publication year - 2004

Publication title -

proceedings of the national academy of sciences

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 5.011

H-Index - 771

eISSN - 1091-6490

pISSN - 0027-8424

DOI - 10.1073/pnas.0403459101

Subject(s) - tubulin , paclitaxel , microtubule , chemistry , anticancer drug , stereochemistry , drug , biophysics , biochemistry , biology , microbiology and biotechnology , pharmacology , chemotherapy , genetics

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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