Oligomerization and allosteric modulation in g -protein coupled receptors /
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| Imprint: | Amsterdam ; Boston : Elsevier/Academic Press, 2013. |
|---|---|
| Description: | 1 online resource (xiii, 471 pages) : illustrations (some color). |
| Language: | English |
| Series: | Progress in molecular biology and translational science, 1877-1173 ; v. 115 Progress in molecular biology and translational science ; v. 115. |
| Subject: | |
| Format: | E-Resource Book |
| URL for this record: | http://pi.lib.uchicago.edu/1001/cat/bib/12378446 |
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| 245 | 0 | 0 | |a Oligomerization and allosteric modulation in g -protein coupled receptors / |c edited by Terry Kenakin. |
| 260 | |a Amsterdam ; |a Boston : |b Elsevier/Academic Press, |c 2013. | ||
| 300 | |a 1 online resource (xiii, 471 pages) : |b illustrations (some color). | ||
| 336 | |a text |b txt |2 rdacontent |0 http://id.loc.gov/vocabulary/contentTypes/txt | ||
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| 490 | 1 | |a Progress in molecular biology and translational science, |x 1877-1173 ; |v v. 115 | |
| 504 | |a Includes bibliographical references and index. | ||
| 505 | 0 | |a Front cover; Oligomerization and Allosteric Modulation in G-Protein Coupled Receptors; Copyright; Contents; Contributors; Preface; Chapter One: Approaches for Probing Allosteric Interactions at 7 Transmembrane Spanning Receptors; 1. Introduction; 2. General Considerations for Assays Designed to Identify and Characterize Allosteric Modulators; 3. General Workflow Used in Identifying and Characterizing Allosteric Modulators; 3.1. High-throughput screening; 3.2. Potency determinations; 3.3. Efficacy determinations; 4. Data Analysis: General Features for Allosteric Interactions. | |
| 505 | 8 | |a 5. Kinetic Assays to Measure Allosteric Interactions at 7TMRs5.1. Fluorescence-based second-messenger assays; 5.2. Calcium mobilization, general principles; 5.3. Thallium flux, general principles; 5.4. Fluorescent probe methodology; 5.5. Alternatives to fluorescence technology; 6. Label-Free Technology; 7. Endpoint Assays; 7.1. cAMP accumulation; 7.2. PI hydrolysis; 7.3. ERK1/2 phosphorylation; 7.4. Arrestin recruitment; 7.5. Transcriptional regulation; 8. Radioligand Binding Assays for Allosteric Interactions; 8.1. General methodology and initial considerations; 8.1.1. Receptor source. | |
| 505 | 8 | |a 8.1.2. Choice of radioligand8.1.3. Experimental conditions; 9. Competitive or Not Competitive; 9.1. Allosteric radioligand competition; 9.2. Orthosteric radioligand competition; 9.3. Dissociation kinetic assays; 10. Conclusions and Future Directions; Acknowledgments; References; Chapter Two: Pharmacology of Metabotropic Glutamate Receptor Allosteric Modulators: Structural Basis and Therapeutic Pote ...; 1. Introduction; 2. Physiology and Pharmacology of mGlus; 2.1. Advantages and complexities of allosteric modulation; 3. Allosteric Modulation of mGlus. | |
| 505 | 8 | |a 3.1. Quantification of allosteric modulation3.2. Verification of an allosteric mechanism of action; 4. Location of Allosteric Sites; 4.1. Structural features of mGlus; 4.2. Localization of allosteric binding sites; 4.3. Common allosteric sites within and between subtypes; 4.4. Multiple allosteric sites within a receptor subtype; 5. Therapeutic Indications for Allosteric Modulators; 5.1. mGlu1 NAMs for neuropathic pain; 5.2. mGlu2/3 PAMs and agonists for schizophrenia and cognition; 5.3. mGlu2/3 in anxiety; 5.4. mGlu2/3 PAMs for drug abuse; 5.5. mGlu2/3 PAMs for depression. | |
| 505 | 8 | |a 5.6. mGlu4 PAMs for PD and neuroprotection5.7. mGlu4 PAMs in pain and neuroinflammation; 5.8. mGlu5 NAMs for anxiety; 5.9. mGlu5 NAMs for major depression disorder; 5.10. mGlu5 NAMs for Autism; 5.11. mGlu5 NAMs for drug abuse; 5.12. mGlu5 NAMs for potential treatment of astrocytic disorders; 5.13. mGlu5 for treatment of PD, iatrogenic dystonias, gastroesophogeal reflux disorder, and migraine; 5.14. mGlu5 PAMs for schizophrenia and cognition; 5.15. mGlu5 PAMs for treatment of TSC; 5.16. mGlu7 for stress and anxiety; 5.17. mGlu8 potential for the treatment of PD and anxiety. | |
| 520 | |a In this thematic volume of <i>Progress in Molecular Biology and Translational Science, </i>researchers reflect on recent developments and research surrounding G protein-coupled receptors. The chapters cover a large breadth of research, including GPCR role in stem cell function and pharmacology. Authors explore in-depth research techniques and applications of GPCR usage, covering theory, laboratory approaches, and unique qualities that make GPCRs a crucial tool in microbiological and cancer research. <br><br> Key features: * Contributions from leading authorities * Informs and updates on. | ||
| 650 | 0 | |a G proteins |x Receptors. | |
| 650 | 7 | |a G proteins |x Receptors. |2 fast |0 (OCoLC)fst00936832 | |
| 655 | 4 | |a Electronic books. | |
| 700 | 1 | |a Kenakin, Terrence P. |0 http://id.loc.gov/authorities/names/n86105077 |1 http://viaf.org/viaf/19854231 | |
| 830 | 0 | |a Progress in molecular biology and translational science ; |v v. 115. |0 http://id.loc.gov/authorities/names/no2009049039 | |
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| 928 | |t Library of Congress classification |a QP552.G16 |l Online |c UC-FullText |u https://www.sciencedirect.com/science/bookseries/18771173/115 |z Elsevier |g ebooks |i 11978490 | ||