Functional Selectivity of G Protein-Coupled Receptor Ligands

• Theoretical and Mechanistic Aspects of Functional Selectivity.- 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.- Subfamilies of Therapeutically Relevant Receptors.- 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.- Functional Selectivity at Non-Opioid Peptide Receptors.

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)