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 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.

Key Features

  • Continues the legacy of this premier serial with quality chapters authored by leaders in the field
  • Covers research methods in biomineralization science
  • Contains sections focusing on protein kinase inhibitors in research and medicine

Readership

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

Table of Contents

  • Preface
  • Chapter One: Catalytic Mechanisms and Regulation of Protein Kinases
    • Abstract
    • 1 Introduction
    • 2 Kinetic Mechanism
    • 3 Chemical Mechanism of Kinase Phosphoryl Transfer
    • 4 Applications of Mechanistic Studies in Understanding Kinase Function and Regulation
    • 5 Summary and Outlook
  • Chapter Two: A Structural Atlas of Kinases Inhibited by Clinically Approved Drugs
    • Abstract
    • 1 Introduction
    • 2 Kinase Structure and Catalytic Mechanism
    • 3 Staurosporine: A Promiscuous ATP-Competitive Inhibitor
    • 4 BCR-Abl Inhibitors
    • 5 Tofacitinib (Xeljanz™) Binds to a “DFG-in” Conformation of Janus Kinase
    • 6 Inhibition of Receptor Tyrosine Kinases
    • 7 Vemurafenib (Zelboraf™) Binds to A “DFG-in” Conformation in the Ser/Thr Kinase RAF
    • 8 Inhibitors That Occupy Pockets Other Than the ATP-Binding Site
    • 9 Summary
    • Acknowledgments
  • Chapter Three: Fragment-Based Approaches to the Discovery of Kinase Inhibitors
    • Abstract
    • 1 Introduction
    • 2 Fragment-Based Drug Discovery
    • 3 Identifying Fragment Hits
    • 4 From Fragments to Leads
    • 5 Alternative Inhibition Strategies
    • 6 Summary
    • Acknowledgments
  • Chapter Four: Targeting Protein Kinases with Selective and Semipromiscuous Covalent Inhibitors
    • Abstract
    • 1 Introduction
    • 2 Design of Irreversible Cysteine-Targeted Kinase Inhibitors
    • 3 Targeting Noncatalytic Cysteines with Reversible Covalent Inhibitors
    • 4 Semipromiscuous Covalent Inhibitors as Chemoproteomic Probes
    • 5 Conclusions and Future Directions
  • Chapter Five: The Resistance Tetrad: Amino Acid Hotspots for Kinome-Wide Exploitation of Drug-Resistant Protein Kinase Alleles
    • Abstract
    • 1 Introduction
    • 2 Protei

Details

No. of pages:
252
Language:
English
Copyright:
© 2014
Published:
Imprint:
Academic Press
Print ISBN:
9780123979186
Electronic ISBN:
9780123984623