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Int. J. Mol. Sci. 2017, 18(8), 1733; doi:10.3390/ijms18081733

Taxol®: The First Microtubule Stabilizing Agent

1
Department of Molecular Pharmacology, Albert Einstein College of Medicine, Bronx, NY 10461, USA
2
Department of Obstetrics and Gynecology and Women’s Health, Division of Gynecologic Oncology, Albert Einstein College of Medicine, Bronx, NY 10461, USA
*
Author to whom correspondence should be addressed.
Received: 20 June 2017 / Revised: 27 July 2017 / Accepted: 28 July 2017 / Published: 9 August 2017
(This article belongs to the Special Issue Microtubule-Targeting Agents)
View Full-Text   |   Download PDF [2134 KB, uploaded 9 August 2017]   |  

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®. View Full-Text
Keywords: Taxol®; drug binding site; photoaffinity labeling; drug resistance; tubulin isotypes Taxol®; drug binding site; photoaffinity labeling; drug resistance; tubulin isotypes
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Yang, C.-P.H.; Horwitz, S.B. Taxol®: The First Microtubule Stabilizing Agent. Int. J. Mol. Sci. 2017, 18, 1733.

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