Academic Press Allosteric Modulation of G Protein-Coupled Receptors

Allosteric Modulation of G Protein-Coupled Receptors reviews fundamental information on G protein-coupled receptors (GPCRs) and allosteric modulation, presenting original research in the area and collectively providing a comprehensive description of key issues in GPCR allosteric modulation. The book provides background on core concepts of molecular pharmacology while also introducing the most important advances and studies in the area. It also discusses key methodologies. This is an essential book for researchers and advanced students engaged in pharmacology, toxicology and pharmaceutical sciences training and research. Many of the GPCR-targeted drugs released in the past decade have specifically worked via allosteric mechanisms. Unlike direct orthosteric-acting compounds that occupy a similar receptor site to that of endogenous ligands, allosteric modulators alter GPCR-dependent signaling at a site apart from the endogenous ligand. Recent methodological and analytical advances have greatly improved our ability to understand the signaling mechanisms of GPCRs. We now know that allostery is a common regulatory mechanism for all GPCRs and not – as we once believed – unique to a few receptor subfamilies. Review Presents recent advances in GPCR allostery and the challenges associated with understanding allosteric modulation as a highly complex approach to GPCR biology From the Back Cover <i>Allosteric Modulation of G Protein-Coupled Receptors</i> reviews fundamental information on G protein-coupled receptors (GPCRs) allosteric modulation and presents original research in the area, which collectively provides a comprehensive description of the key issues in GPCR allosteric modulation. Many of the GPCR-targeted drugs released in the past decade have specifically worked via allosteric mechanisms. Unlike direct orthosteric-acting compounds that occupy a similar receptor site to that of endogenous ligands, allosteric modulators alter GPCR-dependent signalling at a site apart from the endogenous ligand. Recent methodological and analytical advances have greatly improved our ability to understand the signalling mechanisms of GPCRs. We now know that allostery is a common regulatory mechanism for all GPCRs and not – as we once believed – unique to a few receptor subfamilies. Allosteric modulation, whether through small molecules, peptides, or protein-protein interactions, represents a novel and enticing means of affecting GPCR function. But, it is not without its challenges. This book provides background on core concepts of molecular pharmacology while also introducing the most important advances and studies in the area. It also discusses key methodologies. Allosteric Modulation of G Protein-Coupled Receptors is an essential book for researchers and advanced students engaged in pharmacology, toxicology, and pharmaceutical sciences training and research About the Author Robert Laprairie is the GlaxoSmithKline-Canadian Institutes of Health Research chair in Drug Discovery and Development in the College of Pharmacy and Nutrition at the University of Saskatchewan. He currently serves as the President and Director of Education and Trainee Initiatives for the Canadian Consortium for the Investigation of Cannabinoids (CCIC). His teaching responsibilities include basic molecular pharmacology and neuroscience in the undergraduate and graduate Pharmacy programs. He is also involved in committee work with the Canadian Institutes of Health Research and the Animal Research Ethics Board of the University of Saskatchewan. Dr. Laprairie has published more than 50 articles on pharmacology with a focus on the endocannabinoid system and allosteric modulators.