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The Role of Microtubules in Cell Biology, Neurobiology, and Oncology pp 281–306Cite as

Antimicrotubule Agents That Bind Covalently to Tubulin

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Part of the book series: Cancer Drug Discovery and Development ((CDD&D))

Abstract

The binding of most microtubule inhibitors (MTI) is reversible. Most of these inhibit the polymerization of tubulin to microtubules (MT), but an important group promotes polymerization and stabilizes MT. A subset of MTI are not reversible due to covalent adduct formation with tubulin. Some of these agents are quite specific in the amino acid residue targeted for reaction, while others are less specific, though still targeting MT function in cells. Almost all reactive MTI cause loss of MT, but one reactive agent is known that stabilizes MT. Many reactive MTI target cysteines in tubulin, especially in β-tubulin, although MTI are known that target lysine and other residues. Reactive MTI include organic, inorganic, natural, and synthetic compounds, environmental toxicants as well as potential therapeutics.

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Authors and Affiliations

  1. Laboratory of Integrative and Medical Biophysics, National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, MD

    Dan L. Sackett PhD

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  1. Dan L. Sackett PhD
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  1. Medical Oncology Branch, Center for Cancer Research, National Cancer Institute, Bethesda, MD

    Tito Fojo MD, PhD

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© 2008 Humana Press, Totowa, NJ

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Sackett, D.L. (2008). Antimicrotubule Agents That Bind Covalently to Tubulin. In: Fojo, T. (eds) The Role of Microtubules in Cell Biology, Neurobiology, and Oncology. Cancer Drug Discovery and Development. Humana Press. https://doi.org/10.1007/978-1-59745-336-3_12

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  • DOI: https://doi.org/10.1007/978-1-59745-336-3_12

  • Publisher Name: Humana Press

  • Print ISBN: 978-1-58829-294-0

  • Online ISBN: 978-1-59745-336-3

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