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Author: Wayne R. Leifert Publisher: Humana Press ISBN: 9781603273169 Category : Medical Languages : en Pages : 0
Book Description
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, and bio-nanotechnology.
Author: Wayne R. Leifert Publisher: Humana Press ISBN: 9781603273169 Category : Medical Languages : en Pages : 0
Book Description
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, and bio-nanotechnology.
Author: Krishna C. Persaud Publisher: CRC Press ISBN: 1439871728 Category : Medical Languages : en Pages : 237
Book Description
Many advances have been made in the last decade in the understanding of the computational principles underlying olfactory system functioning. Neuromorphic Olfaction is a collaboration among European researchers who, through NEUROCHEM (Fp7-Grant Agreement Number 216916)-a challenging and innovative European-funded project-introduce novel computing p
Author: Publisher: Elsevier ISBN: 0323994326 Category : Science Languages : en Pages : 232
Book Description
G Protein-Coupled Receptors, Part A, Volume 193 in the Progress in Molecular Biology and Translational Science series, highlights new advances in the field. G protein-coupled receptors (GPCRs) represent the largest class of cell surface proteins with an intricate involvement of nearly every physiological process in our body. Approximately, one third of the clinically prescribed medicines target GPCRs and the quest to improve the exiting GPCR-targeting therapeutics continues. These two volumes are focused on activation, signaling and regulation of GPCRs with specific examples of receptor systems and cellular processes. - Covers a broad range of topics related to GPCR activation and signaling - Covers several receptor systems with an emphasis on emerging paradigms - Covers different processes and model systems with a focus on GPCRs
Author: Sofia Aires M. Martins Publisher: Humana ISBN: 9781071612231 Category : Science Languages : en Pages : 327
Book Description
This fully updated edition targets not only those assays directly involved in the discovery of GPCR-active compounds but also those involved in cell-based experiments designed to study physiological responses. Whether coming from academia or industry, or being an experienced researcher or a newcomer to the field, the reader will find accessible methods and protocols that cover the latest developments on receptor purification, molecular biology, recombinant engineering, and analytical techniques that enable the real time monitoring of the complex GPCR signaling cascade and identification of potential drug targets. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Authoritative and up-to-date, G Protein-Coupled Receptor Screening Assays: Methods and Protocols, Second Edition aims to provide the tools necessary to contribute to the advancement of GPCR research and discovery and ultimately lead to the availability of innovative and more efficient drugs.
Author: Tiina P. Iismaa Publisher: Springer Science & Business Media ISBN: 3662219301 Category : Science Languages : en Pages : 189
Book Description
This book is about the recent advances in the structural and functional characterization of receptors that influence intracellular signalling events through interaction with intracellular GTP-binding proteins (G proteins). Molecular cloning of members of the G protein-coupled receptor superfamily has complemented pharmacological investigations in providing a realization of the structural and functional diversity of these receptors. An increased understanding of the involvement of particular receptor subtypes in normal and pathophysiological processes represents exciting possibilities for the development of highly specific and effective therapeutic agents.
Author: Katharine Herrick-Davis Publisher: Humana Press ISBN: 9783319601724 Category : Medical Languages : en Pages : 501
Book Description
G-protein-coupled receptors (GPCRs) are believed to be the largest family of membrane proteins involved in signal transduction and cellular responses. They dimerize (form a pair of macromolecules) with a wide variety of other receptors. The proposed book will provide a comprehensive overview of GPCR dimers, starting with a historical perspective and including, basic information about the different dimers, how they synthesize, their signaling properties, and the many diverse physiological processes in which they are involved. In addition to presenting information about healthy GPCR dimer activity, the book will also include a section on their pathology and therapeutic potentials.
Author: Publisher: Academic Press ISBN: 0123918723 Category : Science Languages : en Pages : 451
Book Description
This new volume of Methods in Enzymology continues the legacy of this premier serial by containing quality chapters authored by leaders in the field. This volume covers G protein coupled receptors and includes chapters on such topics as post-translation modification of GPCR in relationship to biased agonism, structure-based virtual screening, and GPCR oligomerization in the brain. - Continues the legacy of this premier serial with quality chapters authored by leaders in the field - Covers G protein coupled receptors - Contains chapters on such topics as post-translation modification of GPCR in relationship to biased agonism, structure-based virtual screening, and GPCR oligomerization in the brain
Author: Jesús Giraldo Publisher: Royal Society of Chemistry ISBN: 1849731837 Category : Medical Languages : en Pages : 522
Book Description
G protein-coupled receptors (GPCRs) are the largest family of cell-surface receptors, with more than 800 members identified thus far in the human genome. The book lies between the fields of chemical biology, molecular pharmacology, and medicinal chemistry.
Author: Kevin R. Lynch Publisher: John Wiley & Sons ISBN: 9780471194934 Category : Science Languages : en Pages : 246
Book Description
The past decade has seen tremendous advances in the study of G protein-coupled receptors (GPCRs), including the molecular cloning and identification of more than 100 hundred GPCR genes. But while GPCRs serve as targets for more than 300 medicines in the modern pharmacopoeia, the shrinking pool of known ligands and the continuing discovery of orphan GPCR genes have underscored the need for new approaches to ligand identification. Identification and Expression of G Protein-Coupled Receptors addresses this new direction in GPCR biochemistry-offering a definitive laboratory bench manual that emphasizes expression over primary cloning strategies. In a series of expert contributions by well-known researchers, this book provides detailed protocols for various expression systems-from bacteria to mammalian cells-as well as straightforward opinions on the advantages and shortcomings of each approach. Topics covered include: * Homology screening and the polymerase chain reaction in the cloning of GPCR genes * Cloning of GPCRs using mammalian cell expression * GPCR informatics and the orphan problem * The use of Xenopus laevis oocytes for the study of GPCRs * Stable expression of GPCRs in mammalian cells * Heterologous expression in primary cell cultures * Expression of GPCR in Escherichia coli * Large scale expression and purification of GPCRs in mammalian cells * High-level expression of GPCRs in the Baculovirus/Sf9 cell expression system * Expression of GPCRs in Drosophila Schneider 2 cells * Methods for genetic analysis and ligand identification using heterologous GPCRs expressed in Saccharomyces cerevisiae Supplemented with numerous photographs and illustrations, Identification and Expression of G Protein-Coupled Receptors is important reading for biochemists, pharmacologists, neuroscientists, structural biologists, and anyone involved in GPCR-based research. It delivers a wealth of useful advice, practical tips, and invaluable insight into trends at the cutting-edge of current research.
Author: Wayne R. Leifert
Author: Wayne R. Leifert
Author: 
Author: Krishna C. Persaud
Author: 
Author: Sofia Aires M. Martins
Author: Tiina P. Iismaa
Author: Katharine Herrick-Davis
Author: 
Author: Jesús Giraldo
Author: Kevin R. Lynch