Description

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 second 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.

Key Features

  • Second of two volumes focusing on protein kinase inhibitors in research and medicine
  • Part of the Methods in Enzymology serial with authors who are experts in their disciplines

Readership

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

Table of Contents

1. Catalytic Mechanisms and Regulation of Protein Kinases
2. The resistance tetrad: amino acid hotspots for kinome-wide design and exploitation of drug-resistant protein kinase alleles
3. Fragment-based approaches to the discovery of kinase inhibitors
4. FLiK: A Direct Binding Assay for the Identification and Kinetic Characterization of Stabilizers of Inactive Kinase ConformationsFLiK: A Direct Binding Assay for the Identification and Kinetic Characterization of Stabilizers of Inactive Kinase Conformations
5. The Logic and Design of Analog-sensitive (AS) Kinases and their Small Molecule Inhibitors
6. A Structural Atlas of Kinases Inhibited by Clinically Approved Drugs
7. Targeting Protein Kinases with Selective and Semi-Promiscuous Covalent Inhibitors
8. Discovery of Allosteric Bcr-Abl inhibitors from Phenotypic Screen to Clinical Candidate

Details

No. of pages:
496
Language:
English
Copyright:
© 2014
Published:
Imprint:
Academic Press
Print ISBN:
9780123979438
Electronic ISBN:
9780123984616