Evaluation of the tubulin-bound paclitaxel conformation: Synthesis, biology, and SAR studies of C-4 to C-3′ bridged paclitaxel analogues Academic Article uri icon

Overview

MeSH Major

  • Antineoplastic Agents
  • Paclitaxel
  • Tubulin

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.

publication date

  • February 22, 2007

Research

keywords

  • Academic Article

Identity

Language

  • eng

PubMed Central ID

  • PMC2585518

Digital Object Identifier (DOI)

  • 10.1021/jm061071x

PubMed ID

  • 17263521

Additional Document Info

start page

  • 713

end page

  • 25

volume

  • 50

number

  • 4