Inhibitors of the Ras Superfamily G-proteins, Part B - 1st Edition - ISBN: 9780124201460, 9780124202115

Inhibitors of the Ras Superfamily G-proteins, Part B, Volume 34

1st Edition

Serial Volume Editors: Fuyuhiko Tamanoi Channing J. Der
eBook ISBN: 9780124202115
Hardcover ISBN: 9780124201460
Imprint: Academic Press
Published Date: 25th November 2013
Page Count: 280
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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
    • References
  • Chapter Five. Inhibiting the RAS–PI3K Pathway in Cancer Therapy
    • Abstract
    • 1 Introduction
    • 2 The PI3K Pathway
    • 3 PI3K Inhibitors
    • 4 PI3K Pathway Inhibitors
    • 5 Inhibiting PI3K in Cancer
    • 6 Future Directions
    • References
  • Chapter Six. The RalGEF/Ral Pathway: Evaluating an Intervention Opportunity for Ras Cancers
    • Abstract
    • 1 Introduction
    • 2 RalGEF/Ral Signaling and Cancer: A Rationale for Pathway Inhibition
    • 3 Modes of RalGEF/Ral Pathway Inhibition
    • 4 Conclusion
    • Acknowledgments
    • References
  • Chapter Seven. p21-Activated Kinase Inhibitors
    • Abstract
    • 1 Introduction
    • 2 ATP-competitive PAK Inhibitors
    • 3 Allosteric PAK Inhibitors
    • 4 Conclusions and Outlook
    • References
  • Chapter Eight. Recent Progress in Developing Small Molecule Inhibitors Designed to Interfere with Ras Membrane Association: Toward Inhibiting K-Ras and N-Ras Functions
    • Abstract
    • 1 Introduction
    • 2 Combined Inhibition of FTase and GGTase-I to Inhibit K-Ras and N-Ras
    • 3 ICMT Inhibitors
    • 4 Inhibiting the Interaction of K-Ras and PDEδ
    • 5 Future Prospects
    • Acknowledgments
    • References
  • Chapter Nine. Synthetic Lethal Genetic Screens in Ras Mutant Cancers
    • Abstract
    • 1 Introduction
    • 2 Synthetic Lethality and Its Application in Cancer Research
    • 3 Synthetic Lethality Screen to Find “Achilles’ Heel” of Ras Mutant Cancers
    • 4 Conclusion and Perspectives
    • Acknowledgments
    • References
  • Author Index
  • Subject Index


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


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


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© Academic Press 2013
Academic Press
eBook ISBN:
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Ratings and Reviews

About the Serial Volume Editors

Fuyuhiko Tamanoi Serial Volume Editor

Fuyu Tamanoi is a biochemist who has served on the UCLA School of Medicine and UCLA College faculty since he joined the Department of Microbiology, Immunology & Molecular Genetics in 1993. He became a full professor in 1997. Since 1996, he has been a Director of Signal Transduction Program Area at Jonsson Comprehensive Cancer Center. Dr. Tamanoi earned his B.S. and M.S. in Biochemistry at the University of Tokyo. He received PhD in Molecular Biology at Nagoya University in 1977. He was a postdoctoral fellow at Harvard Medical School, where he worked on bacteriophage DNA replication. From 1980 to 1985, he was a senior staff investigator at Cold Spring Harbor Laboratory, where he worked on adenovirus DNA replication. From 1985 to 1993, he was an Assistant Professor and then Associate Professor at the University of Chicago, where he initiated studies on lipid modification of the Ras family proteins. His laboratory research centers on signal transduction and signal transduction inhibitors. He is currently exploring ways to deliver signal transduction inhibitors using nanoparticles.

Affiliations and Expertise

Professor and Vice Chair, Department of Microbiology, Immunology and Molecular Genetics, University of California, Los Angeles and Director, Signal Transduction Program Area, Jonsson Comprehensive Cancer Center, USA

Channing J. Der Serial Volume Editor

Affiliations and Expertise

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