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Int. J. Mol. Sci. 2017, 18(8), 1733;

Taxol®: The First Microtubule Stabilizing Agent

Department of Molecular Pharmacology, Albert Einstein College of Medicine, Bronx, NY 10461, USA
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)
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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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