G Protein-Coupled Receptors in Drug Discovery [electronic resource] / edited by Wayne R. Leifert.
| Call Number | 615 |
| Title | G Protein-Coupled Receptors in Drug Discovery edited by Wayne R. Leifert. |
| Physical Description | XII, 376 p. online resource. |
| Series | Methods in Molecular Biology, Methods and Protocols, 1064-3745 ; 552 |
| Contents | New Insights into GPCR Function: Implications for HTS -- Screening Technologies for G Protein-Coupled Receptors: From HTS to uHTS -- GPCR Signaling: Understanding the Pathway to Successful Drug Discovery -- An Overview on GPCRs and Drug Discovery: Structure-Based Drug Design and Structural Biology on GPCRs -- Understanding the Ligand–Receptor–G Protein Ternary Complex for GPCR Drug Discovery -- Assay Data Quality Assessment -- Homology Modeling of GPCRs -- GPCR Expression Using Baculovirus-Infected Sf9 Cells -- Radioligand Binding Assays: Application of [125I]Angiotensin II Receptor Binding -- [35S]GTP?S Binding in G Protein-Coupled Receptor Assays -- A Time-Resolved Fluorescent Lanthanide (Eu)-GTP Binding Assay for Chemokine Receptors as Targets in Drug Discovery -- Use of the DiscoveRx Hithunter cAMPII Assay for Direct Measurement of cAMP in Gs and Gi GPCRs -- Use of Aequorin for G protein-Coupled Receptor Hit Identification and Compound Profiling -- BacMam: Versatile Gene Delivery Technology for GPCR Assays -- Yeast Assays for G Protein-Coupled Receptors -- GPCR Microspot Assays on Solid Substrates -- Resonant Waveguide Grating Biosensor for Whole-Cell GPCR Assays -- FRET-Based Measurement of GPCR Conformational Changes -- FLIPR® Assays of Intracellular Calcium in GPCR Drug Discovery -- Use of Fluorescence Indicators in Receptor Ligands -- Application of Fluorescence Resonance Energy Transfer Techniques to Establish Ligand–Receptor Orientation -- Detection of GPCR/?-Arrestin Interactions in Live Cells Using Bioluminescence Resonance Energy Transfer Technology -- Using Reporter Gene Technologies to Detect Changes in cAMP as a Result of GPCR Activation -- A Quantum Dot-Labeled Ligand–Receptor Binding Assay for G Protein-Coupled Receptors Contained in Minimally Purified Membrane Nanopatches -- Xenopus Oocyte Electrophysiology in GPCR Drug Discovery -- Immunoprecipitation and Phosphorylation of G Protein-Coupled Receptors. |
| Summary | The G protein-coupled receptors (GPCRs), known to be one of the largest superfamilies in the human genome, underpin a multitude of physiological processes and represent a significant target for bioactive and drug discovery programs. In G Protein-Coupled Receptors in Drug Discovery: Methods and Protocols, experts in the field provide a range of classic and cutting-edge laboratory protocols developed for GPCR research, as well as several current review articles relevant to the area of high throughput GPCR screening, with discussion on GPCR structure and GPCR signalling. Written in the highly successful Methods in Molecular Biology™ series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible protocols, and notes on troubleshooting and avoiding known pitfalls. Authoritative and easy to use, G Protein-Coupled Receptors in Drug Discovery: Methods and Protocols serves to aid all those who wish to further the vital research in their GPCR drug discovery programs. |
| Added Author | Leifert, Wayne R. editor. SpringerLink (Online service) |
| Subject | MEDICINE. PHARMACOLOGY. Biomedicine. Pharmacology/Toxicology. |
| Multimedia |
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| Summary | The G protein-coupled receptors (GPCRs), known to be one of the largest superfamilies in the human genome, underpin a multitude of physiological processes and represent a significant target for bioactive and drug discovery programs. In G Protein-Coupled Receptors in Drug Discovery: Methods and Protocols, experts in the field provide a range of classic and cutting-edge laboratory protocols developed for GPCR research, as well as several current review articles relevant to the area of high throughput GPCR screening, with discussion on GPCR structure and GPCR signalling. Written in the highly successful Methods in Molecular Biology™ series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible protocols, and notes on troubleshooting and avoiding known pitfalls. Authoritative and easy to use, G Protein-Coupled Receptors in Drug Discovery: Methods and Protocols serves to aid all those who wish to further the vital research in their GPCR drug discovery programs. |
| Contents | New Insights into GPCR Function: Implications for HTS -- Screening Technologies for G Protein-Coupled Receptors: From HTS to uHTS -- GPCR Signaling: Understanding the Pathway to Successful Drug Discovery -- An Overview on GPCRs and Drug Discovery: Structure-Based Drug Design and Structural Biology on GPCRs -- Understanding the Ligand–Receptor–G Protein Ternary Complex for GPCR Drug Discovery -- Assay Data Quality Assessment -- Homology Modeling of GPCRs -- GPCR Expression Using Baculovirus-Infected Sf9 Cells -- Radioligand Binding Assays: Application of [125I]Angiotensin II Receptor Binding -- [35S]GTP?S Binding in G Protein-Coupled Receptor Assays -- A Time-Resolved Fluorescent Lanthanide (Eu)-GTP Binding Assay for Chemokine Receptors as Targets in Drug Discovery -- Use of the DiscoveRx Hithunter cAMPII Assay for Direct Measurement of cAMP in Gs and Gi GPCRs -- Use of Aequorin for G protein-Coupled Receptor Hit Identification and Compound Profiling -- BacMam: Versatile Gene Delivery Technology for GPCR Assays -- Yeast Assays for G Protein-Coupled Receptors -- GPCR Microspot Assays on Solid Substrates -- Resonant Waveguide Grating Biosensor for Whole-Cell GPCR Assays -- FRET-Based Measurement of GPCR Conformational Changes -- FLIPR® Assays of Intracellular Calcium in GPCR Drug Discovery -- Use of Fluorescence Indicators in Receptor Ligands -- Application of Fluorescence Resonance Energy Transfer Techniques to Establish Ligand–Receptor Orientation -- Detection of GPCR/?-Arrestin Interactions in Live Cells Using Bioluminescence Resonance Energy Transfer Technology -- Using Reporter Gene Technologies to Detect Changes in cAMP as a Result of GPCR Activation -- A Quantum Dot-Labeled Ligand–Receptor Binding Assay for G Protein-Coupled Receptors Contained in Minimally Purified Membrane Nanopatches -- Xenopus Oocyte Electrophysiology in GPCR Drug Discovery -- Immunoprecipitation and Phosphorylation of G Protein-Coupled Receptors. |
| Subject | MEDICINE. PHARMACOLOGY. Biomedicine. Pharmacology/Toxicology. |
| Multimedia |