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Tubulin-Binding Agents

Synthetic, Structural and Mechanistic Insights

  • Teresa Carlomagno

Part of the Topics in Current Chemistry book series (TOPCURRCHEM, volume 286)

Table of contents

  1. Front Matter
    Pages i-xi
  2. B. Pfeiffer, C.N. Kuzniewski, C. Wullschleger, K.-H. Altmann
    Pages 1-72
  3. I. Paterson, G. J. Florence
    Pages 73-119
  4. Víctor M. Sánchez-Pedregal, Christian Griesinger
    Pages 151-208
  5. Maurizio Botta, Stefano Forli, Matteo Magnani, Fabrizio Manetti
    Pages 279-328
  6. Back Matter
    Pages 329-331

About this book

Introduction

reviews. The SAR data are discussed in light of the structural information available for each agent. The second chapter focuses on the total synthesis of the marine sponge-derived polyketide discodermolide. A comprehensive survey of the synthetic chemistry efforts of several groups over a 14-year period is provided together with a compa- son of the different approaches. The third chapter describes a comprehensive study of the mechanisms of activity of microtubules stabilizing drugs. Thermodynamic, kinetic, structural and fu- tional data on microtubules stabilizing drugs are discussed in an interdisciplinary manner to generate a “time-resolved” picture of the interaction of the drugs with different tubulin forms. The fourth and fifth chapters review the efforts and achievements made in the characterization of the structure of the complexes of tubulin with microtubules stabilizing agents by NMR (Chapter 4) and EM (Chapter 5). Especially evident is the discrepancy of the results obtained for epothilones, where the two techniques deliver radically different structures of the bound drug. Both NMR and EM models are, however, able to explain a consistent set of SAR data. The authors of the two chapters discuss critically the advantages and limitations of each methodology.

Keywords

Biochemistry Destabilizing Agents Microtubules Stabilizing Agents Tubulin-Binding Agents chemistry molecular modelling organic chemistry synthesis

Editors and affiliations

  • Teresa Carlomagno
    • 1
  1. 1.Laboratory (EMBL)European Molecular BiologyHeidelbergGermany

Bibliographic information

  • DOI https://doi.org/10.1007/978-3-540-69039-9
  • Copyright Information Springer-Verlag Berlin Heidelberg 2009
  • Publisher Name Springer, Berlin, Heidelberg
  • eBook Packages Chemistry and Materials Science
  • Print ISBN 978-3-540-69036-8
  • Online ISBN 978-3-540-69039-9
  • Series Print ISSN 0340-1022
  • Series Online ISSN 1436-5049
  • Buy this book on publisher's site