Chapter 3. The Proteasome as a Drug Target

  1. Dr. Robert E. Babine and
  2. Dr. Sherin S. Abdel-Meguid
  1. Tsunehiro Mizushima1 and
  2. Tomitake Tsukihara2

Published Online: 20 FEB 2004

DOI: 10.1002/3527601872.ch3

Protein Crystallography in Drug Discovery

Protein Crystallography in Drug Discovery

How to Cite

Mizushima, T. and Tsukihara, T. (2003) The Proteasome as a Drug Target, in Protein Crystallography in Drug Discovery (eds R. E. Babine and S. S. Abdel-Meguid), Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim, FRG. doi: 10.1002/3527601872.ch3

Editor Information

  1. Suntory Pharmaceutical Research Laboratories, LLC, Structural and Computational Chemistry, One Kendall Square, Bldg 700, Cambridge, MA 02139, USA

Author Information

  1. 1

    Japan Science and Technology Corporation, Structure and Function of Biomolecules, 3-18-22 Honkomagome, Bunkyo-ku, Tokyo, 113-0021, Japan

  2. 2

    Institute for Protein Research, Osaka University, 3-2, Yamadaoka, Suita, Osaka 565-0871, Japan

Publication History

  1. Published Online: 20 FEB 2004
  2. Published Print: 27 NOV 2003

Book Series:

  1. Methods and Principles in Medicinal Chemistry

Book Series Editors:

  1. Prof. Dr. Raimund Mannhold4,
  2. Prof. Dr. Hugo Kubinyi5 and
  3. Prof. Dr. Gerd Folkers6

Series Editor Information

  1. 4

    Biomedical Research Center, Molecular Drug Research Group, Heinrich-Heine-Universität, Universitätsstraße 1, 40225 Düsseldorf, Germany

  2. 5

    BASF AG Ludwigshafen, c/o Donnersbergstraße 9, 67256 Weisenheim am Sand, Germany

  3. 6

    Department of Applied Biosciences, ETH Zürich, Winterthurerstr. 190, 8057 Zürich, Switzerland

ISBN Information

Print ISBN: 9783527306787

Online ISBN: 9783527601875



  • proteasome;
  • ubiquitin-proteasome system;
  • 26S proteasome;
  • 20S proteasome;
  • immunoproteasome;
  • inhibitors


This chapter contains sections titled:

  • Introduction

  • The Ubiquitin-Proteasome System

    • Role of the Ubiquitin-Proteasome System

    • 26S Proteasome

    • 20S Proteasome

  • Structure of the 20S Proteasome

    • Active Sites of Eukaryotic 20S Proteasomes

    • Novel Ntn-Hydrolase Active Site of the β7 Subunit

    • Predicted Structure of Immunoproteasome and Substrate Specificities

  • Proteasome Inhibitors

    • Structure of Proteasome Inhibitor Complexes

  • Conclusions