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

1st Edition - November 7, 2013

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  • Editors: Fuyuhiko Tamanoi, Channing J. Der
  • Hardcover ISBN: 9780124201460
  • eBook ISBN: 9780124202115

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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
      • 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

Product details

  • No. of pages: 280
  • Language: English
  • Copyright: © Academic Press 2013
  • Published: November 7, 2013
  • Imprint: Academic Press
  • Hardcover ISBN: 9780124201460
  • eBook ISBN: 9780124202115

About the Serial Volume Editors

Fuyuhiko Tamanoi

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.

Affiliations and Expertise

Biochemist, Department of Microbiology, Immunology and Molecular Genetics, University of California, Los Angeles, USA

Channing J. Der

Affiliations and Expertise

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

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