(Ebook) Inhibitors of the Ras superfamily G proteins Part B 1st Edition by Fuyuhiko Tamanoi, Channing Der ISBN 9780124201460 0124201466

(Ebook) Inhibitors of the Ras superfamily G proteins Part B 1st Edition by Fuyuhiko Tamanoi, Channing Der ISBN 9780124201460 0124201466

(Ebook) Inhibitors of the Ras superfamily G-proteins, Part B 1st Edition by Fuyuhiko Tamanoi, Channing J. Der  - Ebook PDF Instant Download/Delivery: 9780124201460,  0124201466
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Product details: 

ISBN 10: 0124201466

ISBN 13: 9780124201460

Author: Fuyuhiko Tamanoi, Channing J. Der

Table of contents: 

• 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

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Tags: Fuyuhiko Tamanoi, Channing Der, the Ras superfamily, G proteins