Oligomerization and allosteric modulation in G-protein coupled receptors [electronic resource] / edited by Terry Kenakin.

Oxford : Academic Press, 2013.
1 online resource (495 p.)
1st ed.
Progress in molecular biology and translational science, 1877-1173 ; v. 115

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G proteins -- Receptors.
Allosteric regulation.
Electronic books.
In this thematic volume of Progress in Molecular Biology and Translational Science, 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. Key features: * Contributions from leading authorities * Informs an
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
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
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
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
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
6. Concluding Remarks
Description based upon print version of record.
Includes bibliographical references and index.
Kenakin, Terrence P.