2. Academic Validation
  3. Evaluation of the tubulin-bound paclitaxel conformation: synthesis, biology, and SAR studies of C-4 to C-3' bridged paclitaxel analogues

Evaluation of the tubulin-bound paclitaxel conformation: synthesis, biology, and SAR studies of C-4 to C-3' bridged paclitaxel analogues

  • J Med Chem. 2007 Feb 22;50(4):713-25. doi: 10.1021/jm061071x.
Thota Ganesh 1,  Chao Yang,  Andrew Norris,  Tom Glass,  Susan Bane,  Rudravajhala Ravindra,  Abhijit Banerjee,  Belhu Metaferia,  Shala L Thomas,  Paraskevi Giannakakou,  Ana A Alcaraz,  Ami S Lakdawala,  James P Snyder,  David G I Kingston
Affiliations

Affiliation

  • 1 Department of Chemistry, M/C 0212, Virginia Polytechnic Institute and State University, Blacksburg, Virginia 24061, USA.
PMID: 17263521 DOI: 10.1021/jm061071x
Abstract

The important Anticancer drug paclitaxel binds to the beta-subunit of the alphabeta-tubulin dimer in the microtubule in a stoichiometric ratio, promoting microtubule polymerization and stability. The conformation of microtubule-bound drug has been the subject of intense study, and various suggestions have been proposed. In previous work we presented experimental and theoretical evidence that paclitaxel adopts a T-shaped conformation when it is bound to tubulin. In this study we report additional experimental data and calculations that delineate the allowable parameters for effective paclitaxel-tubulin interactions.

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