Taxol®: The first microtubule stabilizing agent

Research output: Contribution to journalReview article

29 Scopus citations

Abstract

Taxol®, an antitumor drug with significant activity, is the first microtubule stabilizing agent described in the literature. This short review of the mechanism of action of Taxol® emphasizes the research done in the Horwitz’ laboratory. It discusses the contribution of photoaffinity labeled analogues of Taxol® toward our understanding of the binding site of the drug on the microtubule. The importance of hydrogen/deuterium exchange experiments to further our insights into the stabilization of microtubules by Taxol® is addressed. The development of drug resistance, a major problem that arises in the clinic, is discussed. Studies describing differential drug binding to distinct β-tubulin isotypes are presented. Looking forward, it is suggested that the β-tubulin isotype content of a tumor may influence its responses to Taxol®.

Original languageEnglish (US)
Article number1733
JournalInternational Journal of Molecular Sciences
Volume18
Issue number8
DOIs
StatePublished - Aug 10 2017

Keywords

  • Drug binding site
  • Drug resistance
  • Photoaffinity labeling
  • Taxol®
  • Tubulin isotypes

ASJC Scopus subject areas

  • Catalysis
  • Molecular Biology
  • Computer Science Applications
  • Spectroscopy
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry

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