G Protein-Coupled Receptors Structure, Function, and Ligand Screening

With contributions from international experts in the fields of pharmacology, neuroscience, and biochemistry, this text provides an in-depth exploration of GPCRs. Coverage includes the screening of ligands for GPCRs, physiological and molecular characterizations of GPCRs, and structures of GPCRs and their ligands. The book explores current research issues in the post-genome era, particularly the identification of endogenous ligands that may lead to finding new hormones or neurotransmitters. It also discusses the determination of the tertiary structure of GPCRs, useful for understanding GPCR interactions and for the theoretical modeling of drugs.

This book provides a broad base of knowledge of G-protein-coupled receptors. Useful at both the university and industrial levels, this book is of particular interest to those who are developing therapeutic approaches to diseases using drugs that influence receptor activation.

Screening of Ligands for GPCRs. Screening of Endogenous Ligands for Orphan GPCRs. Screening of Ligands for Human GPCRs by the Use of Receptor-Ga Fusion Proteins. Screening and Identification of Ghrelin, an Endogenous Ligand for the Growth-Hormone-Secretagogue Receptor. Ligand Screening of Olfactory Receptors. Functions and Regulation of GPCRs. Generation and Phenotypical Analysis of Muscarinic Acetylcholine Receptor Knockout Mice. Systematic Mutagenesis of M1 Muscarinic Acetylcholine Receptors. Analysis of the Regulation of Muscarinic Acetylcholine Receptors. Single-Molecule Analysis of Chemotactic Signaling Mediated by cAMP Receptor on Living Cells. Oligomerization of G Protein-Coupled Purinergic Receptors. Tertiary Structure of GPCRs and their Ligands. Methods and Results in X-ray Crystallography of Bovine Rhodopsin. Determination of Steric Structure of Muscarinic Ligands Bound to Muscarinic Acetylcholine Receptors: Approaches by TRNOE (Transferred Nuclear Overhauser Effect). Modeling of G Protein-Coupled Receptors for Drug Design.

Tatsuya Haga, Shigeki Takeda