Chapter 6. Molecular Recognition of the Colchicine Binding Site as a Design Paradigm for the Discovery and Development of Vascular Disrupting Agents

  1. Dietmar W. Siemann2,3
  1. Kevin G. Pinney

Published Online: 31 MAY 2006

DOI: 10.1002/0470035439.ch6

Vascular-Targeted Therapies in Oncology

Vascular-Targeted Therapies in Oncology

How to Cite

Pinney, K. G. (2006) Molecular Recognition of the Colchicine Binding Site as a Design Paradigm for the Discovery and Development of Vascular Disrupting Agents, in Vascular-Targeted Therapies in Oncology (ed D. W. Siemann), John Wiley & Sons, Ltd, Chichester, UK. doi: 10.1002/0470035439.ch6

Editor Information

  1. 2

    Shands Cancer Center, University of Florida, Gainsville, Florida, USA

  2. 3

    Research Department of Radiation Oncology, University of Florida, 2000 RW Archer Road, Gainsville, FL 32610, USA

Author Information

  1. Department of Chemistry and Biochemistry, The Center for Drug Discovery, Baylor University, One Bear Place #97348, Waco, TX 76798-7348, USA

Publication History

  1. Published Online: 31 MAY 2006
  2. Published Print: 10 MAR 2006

ISBN Information

Print ISBN: 9780470012949

Online ISBN: 9780470035436

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Keywords:

  • successful molecular architecture;
  • tubulin/microtubule protein system - drug intervention target;
  • vascular disruption;
  • molecular recognition of colchicine binding site;
  • colchicine binding site on tubulin;
  • small-molecule inhibitor of tubulin assembly;
  • vascular disruption therapy;
  • small-molecule VDAs in phase I, Ib and II clinical trials

Summary

This chapter contains sections titled:

  • Introductory comments

  • Colchicine binding site on tubulin

  • Brief overview of tubulin biology

  • Small-molecule inhibitors of tubulin assembly

  • Design paradigm for small-molecule vascular disrupting agents

  • Concluding remarks

  • Acknowledgments

  • References