Description

Targeted toward researchers in biochemistry, molecular and cell biology, pharmacology, and cancer, this is the second part of The Enzymes' volumes that discuss inhibitors of the Ras superfamily G-proteins.

Key Features

  • Informs and updates on all the latest developments in the field
  • Contributions from leading authorities and industry experts

Readership

Researchers in biochemistry, molecular and cell biology, pharmacology, and cancer

Table of Contents

  • Preface
  • Chapter One. Discovery of Small-Molecule Ras Inhibitors that Display Antitumor Activity by Interfering with Ras·GTP–Effector Interaction
    • Abstract
    • 1 Introduction
    • 2 Discovery of Surface Pockets in Novel Crystal Structures of Ras·GTP
    • 3 Discovery of the Kobe0065-Family Compounds by In Silico Screening
    • 4 Inhibition of Ras Functions by the Kobe0065-Family Compounds
    • 5 Structural Basis for Inhibition of Ras Functions by the Kobe0065-Family Compounds
    • 6 Specificity of the Kobe0065-Family Compounds Toward Various Small GTPases
    • 7 Discussion and Conclusion
    • Acknowledgments
    • References
  • Chapter Two. An Orthosteric Inhibitor of the RAS–SOS Interaction
    • Abstract
    • 1 Introduction
    • 2 RAS Signaling in Normal Physiology and Malignancy
    • 3 Strategies for Targeting RAS Activity
    • 4 Inhibitor Design
    • 5 RAS Binding
    • 6 Cell Entry and Intracellular Effects
    • 7 Conclusions
    • References
  • Chapter Three. Conformation-Specific Inhibitors of Raf Kinases
    • Abstract
    • 1 Introduction
    • 2 Kinase Conformations and Different Types of Kinase Inhibitors
    • 3 Representative Raf Inhibitors and Their Binding Modes
    • 4 Raf Kinase Dimerization and Activation
    • 5 Perspective
    • 6 Conclusion
    • Acknowledgments
    • References
  • Chapter Four. Inhibitors of the ERK Mitogen-Activated Protein Kinase Cascade for Targeting RAS Mutant Cancers
    • Abstract
    • 1 Introduction
    • 2 Ras and the ERK MAPK Effector Signaling Network
    • 3 Role of the ERK MAPK Cascade in Mutant RAS-Dependent Tumor Progression and Maintenance
    • 4 MEK1/2 Inhibitors
    • 5 ERK1/2 Inhibitors
    • 6 Issues and Questions
    • Acknowledgments
    • Refere

Details

No. of pages:
280
Language:
English
Copyright:
© 2013
Published:
Imprint:
Academic Press
Print ISBN:
9780124201460
Electronic ISBN:
9780124202115