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
eBook ISBN:
9780124202115
Print ISBN:
9780124201460

About the serial-volume-editors

Fuyuhiko Tamanoi

Professor Fuyu Tamanoi works at the Dept. of Microbiology, Immunology and Molecular Genetics at the University of California.

Affiliations and Expertise

University of California, Los Angeles, USA

Channing J. Der

Affiliations and Expertise

University of North Carolina at Chapel Hill, Chapel Hill, USA