Protein Kinase Inhibitors in Research and Medicine

Edited by

  • Kevan Shokat, Department Cellular and Molecular Pharmacology, University of California San Francisco, CA, USA

This new volume of Methods in Enzymology continues the legacy of this premier serial with quality chapters authored by leaders in the field. This volume covers protein kinase inhibitors in research and medicine, and includes chapters on such topics as fragment-based screening, broad kinome profiling of kinase inhibitors, and designing drug-resistant kinase alleles.
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Audience

Biochemists, biophysicists, molecular biologists, analytical chemists, and physiologists

 

Book information

  • Published: November 2014
  • Imprint: ACADEMIC PRESS
  • ISBN: 978-0-12-397918-6

Reviews

This new volume of Methods in Enzymology continues the legacy of this premier serial with quality chapters authored by leaders in the field. This is the first of two volumes covering protein kinase inhibitors in research and medicine, and includes chapters on such topics as fragment based screening, broad kinome profiling of kinase inhibitors, and designing drug resistant kinase alleles.




Table of Contents

1. Catalytic Mechanisms and Regulation of Protein Kinases
Zhihong Wang and Philip A. Cole.
2. A Structural Atlas of Kinases Inhibited by Clinically Approved Drugs
Qi Wang, Julie A. Zorn and John Kuriyan.
3. Fragment-Based Approaches to the Discovery of Kinase Inhibitors
Paul N. Mortenson, Valerio Berdini and Marc O’Reilly.
4. Targeting Protein Kinases with Selective and Semi-Promiscuous Covalent Inhibitors
Rand M. Miller and Jack Taunton.
5. The Resistance Tetrad: Amino Acid Hotspots for Kinome-Wide Exploitation of Drug-resistant Protein Kinase Alleles
Veselin I Andreev and Patrick A Eyers
6. FLiK: A Direct Binding Assay for the Identification and Kinetic Characterization of Stabilizers of Inactive Kinase Conformations
Jeffrey R. Simar and Daniel Rauh
7. Discovery of Allosteric Bcr-Abl inhibitors from Phenotypic Screen to Clinical Candidate
Nathanael S. Gray and Doriano Fabbro
8. The Logic and Design of Analog-Sensitive (AS) Kinases and their Small Molecule Inhibitors
Michael S. Lopez, Joseph Kliegman and Kevan M. Shokat