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    Proc Natl Acad Sci U S A. 2004 Jul 6;101(27):10006-11. Epub 2004 Jun 28.

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

    Ganesh T, Guza RC, Bane S, Ravindra R, Shanker N, Lakdawala AS, Snyder JP, Kingston DG.

    Department of Chemistry, M/C 0212, Virginia Polytechnic Institute and State University, Blacksburg, VA 24061, USA.

    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.

    PMID: 15226503 [PubMed - indexed for MEDLINE]

    PMCID: 454156

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