G Protein-Coupled Receptors in Drug Discovery
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Beschreibung
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.
The G protein-coupled receptors (GPCRs) and associated peripheral G proteins underpin a multitude of physiological processes. The GPCRs represent one of the largest superfamilies in the human genome and are a significant target for bioactive and drug discovery programs. It is estimated that greater than 50% of all drugs, including those in development, currently target GPCRs. Many of the characterized GPCRs have known ligands; however, approximately 20% of GPCRs are described as orphan GPCRs, apparent GPCRs that share the generic high-level structure charact- istic of GPCRs but whose endogenous ligand is not known. Therefore, it is expected that the field of GPCR drug discovery and development will greatly expand in the coming years with emphasis on new generations of drugs against GPCRs with unique therapeuticuseswhichmayincludedrugssuchasallostericregulators,inverseagonists, and identification of orphan GPCR ligands. AswelearnmoreaboutthemolecularsignalingcascadesfollowingGPCRactivation, we acquire a better appreciation of the complexity of cell signaling and as a result, also acquire a vast array ofnew molecularmethods toinvestigate these andother processes. Thegeneralaimofthisbookistoprovideresearcherswitharangeofprotocolsthatmay be useful in their GPCR drug discovery programs. It is also the basis for the devel- ment of future assays in this field. Therefore, the range of topics covered and the appropriate methodological approaches in GPCR drug discovery are reflected in this book. Itisinterestingtonotethatfuturedirectionsindrugdiscoverywillrequireinput and collaboration from a plethora of fields of research. As such, this book will likely be of interest to scientists involved in such fields as molecular biology, pharmacology, biochemistry, cellular signaling, andbio-nanotechnology.
Contains several comprehensive reviews of GPCR screening technologies by authoritative 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 throughput screening and research-based, high information content assays Presents a diverse approach to experimental design, covering model biological systems, screening modalities, detection technologies, and approaches to data analysis Comprehensive guide to developing, running, and analyzing cell-based assays in high-throughput screening Includes supplementary material: sn.pub/extras
Autor*in
Wayne R. Leifert
Themen in »G Protein-Coupled Receptors in Drug Discovery«
Calcium Cellular signalling Chemokine Drug development GPCRs Ligands physiology
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From the reviews:
“To fully understand the GPCR drug discovery process one should … have wide knowledge of the methods/protocols used in this process. This book serves this exact purpose. … It’s biggest strength is a clear description of every aspect of GPCR drug discovery process, which is easy to understand even for a non-expert in the respective field. … a must-read for everyone involved in GPCR drug discovery and particularly for scientists working in multidisciplinary teams, who need to soundly communicate ideas with experts in other fields.” (Bartosz Trzaskowski, Acta Biochimica Polonica, Vol. 56, December, 2009)
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