(EBOOK PDF)Inhibitors of the Ras superfamily G proteins Part B 1st Edition by Fuyuhiko Tamanoi, Channing Der 9780124201460 0124201466 full chapters

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• ISBN 10:0124201466 

• ISBN 13:9780124201460

• Author:Fuyuhiko Tamanoi, Channing Der  

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

* Contributions from leading authorities

* Informs and updates on all the latest developments in the field

                                                                                                                                                 

Inhibitors of the Ras superfamily G proteins Part B 1st 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
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