edited by R.E. Babine
and S.S. Abdel-Meguid

In Protein Crystallography in Drug Discovery, researchers from academia and from leading pharmaceutical companies present valuable first-hand information on how to obtain the desired protein structures and how to exploit crystallographic data for the drug discovery process.

Covers:

• Crystallography of important target classes such as kinases and proteases
• Structure-based design of protease inhibitors
• Structure-based design of kinase inhibitors
• The ribosome and the proteasome as drug targets
• Recent methodological advances in high-throughput crystallography and microcrystallization

Protein Crystallography in Drug Discovery is an indispensable companion for crystallographers involved in protein structure determination as well as drug developers following the structure-based approach.

Contents

1. Molecular Recognition of Nuclear Hormone Receptor-Ligand Complexes
2. Kinases
3. The Proteasome as a Drug Target
4. Antibiotics and the Ribosome
5. Structure-Based Design of Cathepsin K Inhibitors
6. Structure-Based Design of Potent and Selective Cdk4 Inhibitors
7. Crystallization and Analysis of Serine Proteases with Ecotin
8. X-ray Crystallography in the Development of Orthogonal Ligand-Receptor Pairs
9. Engineering Proteins to Promote Crystallization
10. High-throughput Crystallography
11. Micro-Crystallization

Subject Index

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