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Inhibitors of the Ras Superfamily G-proteins, Part B
1st Edition - November 7, 2013
Editors: Fuyuhiko Tamanoi, Channing J. Der
Hardback ISBN:9780124201460
9 7 8 - 0 - 1 2 - 4 2 0 1 4 6 - 0
eBook ISBN:9780124202115
9 7 8 - 0 - 1 2 - 4 2 0 2 1 1 - 5
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… Read more
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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.
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
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
No. of pages: 280
Language: English
Published: November 7, 2013
Imprint: Academic Press
Hardback ISBN: 9780124201460
eBook ISBN: 9780124202115
FT
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
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Channing J. Der
Affiliations and expertise
University of North Carolina at Chapel Hill, Chapel Hill, USA