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. Contains several comprehensive reviews of GPCR screening technologies byauthoritative leaders Provides an easily accessible reference volume for cell-based GPCR screening written by leading researchers in the field Covers a wide range of assay formats and systems Emphasizes technologies applicable to high throuput screening and research-based, high information content assays INDICE: From the 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]GTPg S Binding in G-Protein Coupled Receptor Assays.- A Time-Resolved Fluorescent Lanthanide (Eu)-GTP Binding Assay for Chemokine Receptors as Targets inDrug 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.
- ISBN: 978-1-60327-316-9
- Editorial: Humana
- Encuadernacion: Cartoné
- Páginas: 370
- Fecha Publicación: 01/05/2009
- Nº Volúmenes: 1
- Idioma: Inglés