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Molecular Cancer Therapeutics
Molecular Cancer Therapeutics
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Microtubule inhibitors: Differentiating tubulin-inhibiting agents based on mechanisms of action, clinical activity, and resistance

Edith A. Perez
Edith A. Perez
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DOI: 10.1158/1535-7163.MCT-09-0366 Published August 2009
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This article has a correction. Please see:

  • Correction: Microtubule Inhibitors: Differentiating Tubulin-Inhibiting Agents Based on Mechanisms of Action, Clinical Activity, and Resistance - June 10, 2012

Abstract

Microtubules are important cellular targets for anticancer therapy because of their key role in mitosis. Microtubule inhibitors (MTI) such as taxanes, vinca alkaloids, and epothilones stabilize or destabilize microtubules, thereby suppressing microtubule dynamics required for proper mitotic function, effectively blocking cell cycle progression and resulting in apoptosis. In spite of their antitumor activity, innate or acquired drug resistance to MTIs such as the taxanes is common, limiting their overall clinical efficacy. Further insight into the mechanisms of action of microtubule-targeting drugs has lead to the discovery of novel agents that may provide higher efficacy with limited toxicity and help overcome resistance to conventional MTIs. This review will focus on the different mechanisms of action of MTIs, potential factors related to resistance and tolerability, and will discuss the recent approval as well as the development of new antineoplastic agents. [Mol Cancer Ther 2009;8(8):2086–95]

Footnotes

    • Received April 23, 2009.
    • Accepted April 27, 2009.
  • © 2009 American Association for Cancer Research.
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Molecular Cancer Therapeutics: 8 (8)
August 2009
Volume 8, Issue 8
  • Table of Contents
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Microtubule inhibitors: Differentiating tubulin-inhibiting agents based on mechanisms of action, clinical activity, and resistance
Edith A. Perez
Mol Cancer Ther August 1 2009 (8) (8) 2086-2095; DOI: 10.1158/1535-7163.MCT-09-0366

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Microtubule inhibitors: Differentiating tubulin-inhibiting agents based on mechanisms of action, clinical activity, and resistance
Edith A. Perez
Mol Cancer Ther August 1 2009 (8) (8) 2086-2095; DOI: 10.1158/1535-7163.MCT-09-0366
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  • Article
    • Abstract
    • Introduction
    • Microtubule Structure
    • Microtubule Dynamics
    • Microtubule-Destabilizing Agents
    • Microtubule-Stabilizing Agents
    • Resistance
    • Novel Microtubule Inhibitors in Development
    • Epothilones
    • Epothilone B Analog Ixabepilone
    • Epothilone B (Patupilone, EPO906)
    • Epothilone D and Analogs (KOS-862 and KOS-1584)
    • Vinca Alkaloids, Vinflunine
    • Halichondrin B Analog Erubilin Mesylate
    • Taxane Analog DJ-927
    • Conclusions
    • Disclosure of Potential Conflicts of Interest
    • Footnotes
    • References
  • Figures & Data
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Molecular Cancer Therapeutics
eISSN: 1538-8514
ISSN: 1535-7163

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