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Inhibitors of the Ras superfamily g-proteins. Part A /
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 th...
| Clasificación: | Libro Electrónico |
|---|---|
| Otros Autores: | |
| Formato: | Electrónico eBook |
| Idioma: | Inglés |
| Publicado: |
Waltham, MA :
Academic Press,
2013.
|
| Edición: | First edition. |
| Colección: | Enzymes ;
v. 33. |
| Temas: | |
| Acceso en línea: | Texto completo Texto completo |
MARC
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| 020 | |a 0124169678 |q (electronic bk.) | ||
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| 245 | 0 | 0 | |a Inhibitors of the Ras superfamily g-proteins. |n Part A / |c edited by Fuyuhiko Tamanoi. |
| 250 | |a First edition. | ||
| 264 | 1 | |a Waltham, MA : |b Academic Press, |c 2013. | |
| 300 | |a 1 online resource (361 pages) : |b illustrations (some color) | ||
| 336 | |a text |b txt |2 rdacontent | ||
| 337 | |a computer |b c |2 rdamedia | ||
| 338 | |a online resource |b cr |2 rdacarrier | ||
| 490 | 1 | |a The enzymes, |x 1874-6047 ; |v volume thirty three | |
| 504 | |a Includes bibliographical references and indexes. | ||
| 588 | 0 | |a Online resource; title from PDF title page (ebrary, viewed September 19, 2013). | |
| 505 | 0 | |a Front Cover; Inhibitors of the Ras Superfamily G-proteins, Part A; Copyright; Contents; Preface; Chapter One: The Ras Superfamily G-Proteins; 1. The Ras Superfamily G-Proteins; 2. Overview of Structure, Activity, and Regulatory Proteins; 2.1. Three-dimensional structure; 2.2. GEF and GAP regulate the activities of the Ras superfamily G-proteins; 2.3. Posttranslational modification and membrane association; 3. Upstream and Downstream Signaling Pathways; 4. Significance in Human Cancer; 5. Strategies to Inhibit the Ras Superfamily G-Proteins; Acknowledgments; References | |
| 505 | 8 | |a Chapter Two: NMR Study to Identify a Ligand-Binding Pocket in Ras1. KRAS as a Drug Target; 2. Nuclear Magnetic Resonance Fragment Screen; 2.1. Introduction; 2.2. The design of NMR fragment-screening cascade against KRas4B G12D mutant; 2.3. The fragment library; 2.4. The ligand-based primary screen; 2.5. Hit validation using protein-observed NMR; 2.6. FH2L using Kd determinations based on protein-observed NMR; 3. Protein Ligand Co-structures; 3.1. The crystal structure of KRas4BG12D (KRasm); 3.2. The high-resolution view of ligand and KRasm interaction | |
| 505 | 8 | |a 3.3. The ligand-binding pocket expands upon DCAI binding4. Inhibition of SOS1-Mediated Nucleotide Exchange for RAS; 5. Ligand-Binding Sites on Ras; 6. Summary and Conclusions; References; 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 | |
| 505 | 8 | |a 6. Modulation of the Allosteric States in Ras-GTP by Small Molecules7. Mapping the Binding Site Hot Spots in Ras: Targeting the Protein/Membrane Interface; 8. Conclusions; References; 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 | |
| 520 | |a 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. | ||
| 650 | 0 | |a Ras proteins. | |
| 650 | 0 | |a G proteins. | |
| 650 | 2 | |a ras Proteins |0 (DNLM)D018631 | |
| 650 | 2 | |a GTP-Binding Proteins |0 (DNLM)D019204 | |
| 650 | 6 | |a Prot�eines ras. |0 (CaQQLa)201-0247764 | |
| 650 | 6 | |a Prot�eines G. |0 (CaQQLa)201-0203891 | |
| 650 | 7 | |a SCIENCE |x Life Sciences |x Biochemistry. |2 bisacsh | |
| 650 | 7 | |a G proteins. |2 fast |0 (OCoLC)fst00936830 | |
| 650 | 7 | |a Ras proteins. |2 fast |0 (OCoLC)fst01090194 | |
| 700 | 1 | |a Tamanoi, Fuyuhiko. | |
| 776 | 0 | 8 | |i Print version: |t Inhibitors of the Ras superfamily g-proteins. Part A. |b First edition. |z 0124167497 |z 9780124167490 |
| 830 | 0 | |a Enzymes ; |v v. 33. | |
| 856 | 4 | 0 | |u https://sciencedirect.uam.elogim.com/science/book/9780124167490 |z Texto completo |
| 856 | 4 | 0 | |u https://sciencedirect.uam.elogim.com/science/bookseries/18746047/33 |z Texto completo |