Chapter 7. Crystallization and Analysis of Serine Proteases with Ecotin

  1. Dr. Robert E. Babine and
  2. Dr. Sherin S. Abdel-Meguid
  1. Sandra M. Waugh1 and
  2. Robert J. Fletterick2

Published Online: 20 FEB 2004

DOI: 10.1002/3527601872.ch7

Protein Crystallography in Drug Discovery

Protein Crystallography in Drug Discovery

How to Cite

Waugh, S. M. and Fletterick, R. J. (2003) Crystallization and Analysis of Serine Proteases with Ecotin, 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.ch7

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

    University of California at San Francisco, Graduate Group in Biophysics, San Francisco, CA 94143-2240, USA

  2. 2

    Departments of Biochemistry and Biophysics and Pharmaceutical Chemistry, University of California at San Francisco, 600 16th Street, Box 2240, San Francisco, CA 94143-2240, USA

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

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Keywords:

  • crystallization;
  • serine proteases;
  • ecotin;
  • collagenase;
  • E2P2 complexes

Summary

This chapter contains sections titled:

  • What is Ecotin?

  • Methods

    • Expression of Wild Type Ecotin

    • Purification of Wild Type Ecotin

    • Crystallization of Ecotin and Protease Complexes

  • Representative Examples of Ecotin and Protease Structures

    • Ecotin Defines the S7 Through S4' Subsites of Collagenase

    • Ecotin as a Tight Binding Substrate

    • Ecotin Defines Regions Distal to the Factor Xa Protease Domain

  • Crystallization and Structure Determination of E2P2 Complexes

  • Conclusion