Functional Selectivity of G Protein-Coupled Receptor Ligands: New Opportunities for Drug Discovery

Author:   Kim Neve
Publisher:   Humana Press Inc.
Edition:   Softcover reprint of the original 1st ed. 2009
ISBN:  

9781493961160


Pages:   292
Publication Date:   23 August 2016
Format:   Paperback
Availability:   Manufactured on demand   Availability explained
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Functional Selectivity of G Protein-Coupled Receptor Ligands: New Opportunities for Drug Discovery


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Overview

Functional selectivity refers to the ability of different ligands acting at one receptor subtype to activate multiple signaling pathways in unique combinations; that is, one drug can be an agonist at pathway A and an antagonist or partial agonist at pathway B, and another drug can have the reverse profile. Functional selectivity has profound implications for drug development, for chemical biology, and for the design of experiments to characterize receptor function. In Functional Selectivity of G Protein-Coupled Receptors expert neuroscientists and pharmacologists review the work that demonstrated the existence of functional selectivity, placed it within a theoretical framework, and provided a mechanistic basis for the phenomenon. This exciting, comprehensive, and future-oriented volume includes chapters that focus on theoretical and mechanistic aspects of functional selectivity and that cut across subfamilies of GPCRs. Additional chapters focus on subfamilies of therapeutically relevant receptors where there is considerable evidence of ligand functional selectivity. Accessible and authoritative, Functional Selectivity of G Protein-Coupled Receptors is a valuable educational tool and reference source for students and scientists interested in drug development, chemical biology, and GPCR function.

Full Product Details

Author:   Kim Neve
Publisher:   Humana Press Inc.
Imprint:   Humana Press Inc.
Edition:   Softcover reprint of the original 1st ed. 2009
Dimensions:   Width: 15.50cm , Height: 1.60cm , Length: 23.50cm
Weight:   0.630kg
ISBN:  

9781493961160


ISBN 10:   1493961160
Pages:   292
Publication Date:   23 August 2016
Audience:   Professional and scholarly ,  Professional & Vocational
Format:   Paperback
Publisher's Status:   Active
Availability:   Manufactured on demand   Availability explained
We will order this item for you from a manufactured on demand supplier.

Table of Contents

Historical Overview of the Concept of Functional Selectivity.- Functional Selectivity: Theoretical Considerations and Future Directions.- Agonist Selective Coupling of G Protein-Coupled Receptors.- Ligand-Selective Receptor Desensitization and Endocytosis.- Selectivity for G protein or Arrestin-Mediated Signaling.- In Vivo Evidence for and Consequences of Functional Selectivity.- Functional Selectivity at Adrenergic Receptors.- Signaling Diversity Mediated by Muscarinic Acetylcholine Receptor Subtypes and Evidence for Functional Selectivity.- Functional Selectivity at Serotonin Receptors.- Functional Selectivity at Dopamine Receptors.- Functional Selectivity at Receptors for Cannabinoids and other Lipids.- Functional Selectivity at Opioid Receptors Graciela Piñeyro.- Functional Selectivity at non-Opioid Peptide Receptors

Reviews

From the reviews: This book presents the current status of knowledge about ligand-specific intracellular signaling. This book will be of greatest interest and utility to scientists actively involved in research into G protein-coupled receptors or drug discovery. This is a thorough, and detailed assessment of the current state of knowledge and recent developments in the field of G protein-coupled receptor function, signaling, and pharmacology. (Beth Levant, Doody s Review Service, December, 2009) Gives a comprehensive overview on all aspects of the functional selectivity concept of GPCR ligands . It will help to generate more awareness for a key topic within the research community. the volume at hand is of great educational benefit. In general, the volume under review can be considered an excellent book . can be an excellent companion for researchers just jumping into the field of GPCR agonist research, as well as for the expert scientist in the field. (Christoph Boss, ChemMedChem, Vol. 5, 2010)


From the reviews: This book presents the current status of knowledge about ligand-specific intracellular signaling. ... This book will be of greatest interest and utility to scientists actively involved in research into G protein-coupled receptors or drug discovery. ... This is a ... thorough, and detailed assessment of the current state of knowledge and recent developments in the field of G protein-coupled receptor function, signaling, and pharmacology. (Beth Levant, Doody's Review Service, December, 2009) Gives a comprehensive overview on all aspects of the functional selectivity concept of GPCR ligands ... . It will help to generate more awareness for a key topic within the research community. ... the volume at hand is of great educational benefit. ... In general, the volume under review can be considered an excellent book ... . can be an excellent companion for researchers just jumping into the field of GPCR agonist research, as well as for the expert scientist in the field. (Christoph Boss, ChemMedChem, Vol. 5, 2010)


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