The Epothilones: An Outstanding Family of Anti-Tumor Agents

From Soil to the Clinic

  • Authors
  • K.- H. Altmann
  • G. Höfle
  • R. Müller
  • J. Mulzer
  • K. Prantz

Table of contents

  1. Front Matter
    Pages I-IX
  2. Gerhard Höfle
    Pages 5-28
  3. Johann Mulzer, Kathrin Prantz
    Pages 55-133
  4. Karl-Heinz Altmann
    Pages 135-156
  5. Karl-Heinz Altmann
    Pages 221-237
  6. Back Matter
    Pages 239-260

About this book

Introduction

Epothilones have received unusual attention over the past ten years. They are novel antitumor drugs which very much like their predecessor paclitaxel (Taxol) act via microtubule stabilization. In comparison to paclitaxel and a number of alternative drugs with a similar mode of bioaction (e.g. laulimalide, eleutherobin, peluroside, discodermolide) the epothilones have significant advantages, above all very high activity in the nanomolar range and low susceptibility towards multidrug resistance. Epothilone B and several derivatives thereof are in phase I-III clinical trials; one of them (ixabepilone, BMS) is already on the market, others are supposed to appear on the market in the near future. All naturally occurring epothilones have been isolated from Sorangium cellulosum; their antitumor action is traced back to the stabilization of microtubules. In consequence, the formation of the mitototic spindle is prohibited and the cell undergoes apoptosis.

Keywords

Expression anti-tumour agent anti-tumour drug apoptosis biochemistry chemistry epothilone genetic engineering

Bibliographic information

  • DOI https://doi.org/10.1007/978-3-211-78207-1
  • Copyright Information Springer Vienna 2009
  • Publisher Name Springer, Vienna
  • eBook Packages Chemistry and Materials Science
  • Print ISBN 978-3-211-78206-4
  • Online ISBN 978-3-211-78207-1
  • Series Print ISSN 0071-7886
  • About this book