Inhibitors of the Ras Superfamily G-proteins, Part A, Volume 33

1st Edition

Serial Volume Editors: Fuyuhiko Tamanoi
Hardcover ISBN: 9780124167490
eBook ISBN: 9780124169678
Imprint: Academic Press
Published Date: 27th August 2013
Page Count: 364
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Table of Contents

Chapter One. The Ras Superfamily G-Proteins

1 The Ras Superfamily G-Proteins

2 Overview of Structure, Activity, and Regulatory Proteins

3 Upstream and Downstream Signaling Pathways

4 Significance in Human Cancer

5 Strategies to Inhibit the Ras Superfamily G-Proteins



Chapter Two. NMR Study to Identify a Ligand-Binding Pocket in Ras

1 KRAS as a Drug Target

2 Nuclear Magnetic Resonance Fragment Screen

3 Protein Ligand Co-structures

4 Inhibition of SOS1-Mediated Nucleotide Exchange for RAS

5 Ligand-Binding Sites on Ras

6 Summary and Conclusions


Chapter Three. The Allosteric Switch and Conformational States in Ras GTPase Affected by Small Molecules

1 Introduction

2 Ras Architecture: The G Domain and Its Function

3 The Allosteric Switch in Ras-GTP and Its Role in Intrinsic Hydrolysis

4 The Allosteric Switch Linked to the Ras/Raf/MEK/ERK Pathway

5 Most Ras Structures in the Protein Data Bank are in the R State

6 Modulation of the Allosteric States in Ras-GTP by Small Molecules

7 Mapping the Binding Site Hot Spots in Ras: Targeting the Protein/Membrane Interface

8 Conclusions


Chapter Four. State 1(T) Inhibitors of Activated Ras

1 Introduction

2 Allosteric Regulation of the Ras–Effector Interaction

3 Identification of State 1(T) in Activated Ras by NMR Spectroscopy

4 Identification of 1(T) Inhibitors by NMR Spectroscopy

5 Metal-Cyclen Derivatives as 1(T) Inhibitors

6 Metal-BPA Derivatives as 1(T) Inhibitors

7 Outlook: Possible Applications to Other Small GTPases


Chapter Five. Sugar-Based Inhibitors of Ras Activation: Biological Activity and Identification of Ras–Inhibitor Binding Interface

1 Introduction

2 Initial Compound


This special volume of The Enzymes is targeted toward researchers in biochemistry, molecular and cell biology, pharmacology, and cancer. This thematic volume discusses inhibitors of the Ras superfamily G-proteins.

Key Features

  • Contributions from leading authorities
  • Informs and updates on all the latest developments in the field


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


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© Academic Press 2013
Academic Press
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About the Serial Volume Editors

Fuyuhiko Tamanoi Serial Volume Editor

Professor Fuyu Tamanoi works at the Dept. of Microbiology, Immunology and Molecular Genetics at the University of California.

Affiliations and Expertise

University of California, Los Angeles, USA