A thorough discussion of the structure, pharmacology, function, and role of G protein-coupled receptors In GPCRs as Therapeutic Agents, distinguished researcher Dr. Annette Gilchrist delivers an authoritative and in-depth compendium of a vibrant and active area of academic and industrial drug discovery. The book serves as an important reference for new and experienced researchers studying G protein-coupled receptors and discusses the molecular pharmacology of this important target class. It also includes up-to-date material on GPCR structures and structure-based drug design. The book explores the role of GPCRs in the treatment of disease and novel approaches to their study. In addition to providing information on the structure, pharmacology, and function of GPCRs, it discusses their role in disease states, and advances new methods for measuring GPCR activity in an accessible and engaging way. The book includes: A thorough introduction to the molecular pharmacology of G protein-coupled receptors, including up-to-date material on GPCR structures and structure-based drug design In-depth discussions of the evolving pharmacology for GPCRs, intracellular trafficking, and subcellular GPCR signaling Comprehensive explorations of allosteric modulation, receptor dimerization, deorphanization, and ubiquitination Fulsome treatments of the role played by GPCRs in the treatments of cancer, substance use disorders, cerebrovascular diseases, and metabolic diseasesPerfect for researchers in biochemistry, cell biology, and pharmacology, GPCRs as Therapeutic Agents will also earn a place in the libraries of professionals working in medicinal chemistry, structural biology, and clinical pharmacology.

A thorough discussion of the structure, pharmacology, function, and role of G protein-coupled receptorsIn GPCRs as Therapeutic Agents, distinguished researcher Dr. Annette Gilchrist delivers an authoritative and in-depth compendium of a vibrant and active area of academic and industrial drug discovery. The book serves as an important reference for new and experienced researchers studying G protein-coupled receptors and discusses the molecular pharmacology of this important target class. It also includes up-to-date material on GPCR structures and structure-based drug design.The book explores the role of GPCRs in the treatment of disease and novel approaches to their study. In addition to providing information on the structure, pharmacology, and function of GPCRs, it discusses their role in disease states, and advances new methods for measuring GPCR activity in an accessible and engaging way. The book includes:* A thorough introduction to the molecular pharmacology of G protein-coupled receptors, including up-to-date material on GPCR structures and structure-based drug design* In-depth discussions of the evolving pharmacology for GPCRs, intracellular trafficking, and subcellular GPCR signaling* Comprehensive explorations of allosteric modulation, receptor dimerization, deorphanization, and ubiquitination* Fulsome treatments of the role played by GPCRs in the treatments of cancer, substance use disorders, cerebrovascular diseases, and metabolic diseasesPerfect for researchers in biochemistry, cell biology, and pharmacology, GPCRs as Therapeutic Agents will also earn a place in the libraries of professionals working in medicinal chemistry, structural biology, and clinical pharmacology.

Chapter 1 - An overview of G protein coupled receptors and their signaling partnersChapter 2 - Recent advances in orphan GPCRs research and therapeutic potentialChapter 3 - The Evolution of Our Understanding of GPCRsChapter 4 - Approaching GPCR dimers and higher order oligomers using biophysical, biochemical and proteomic methodsChapter 5 - Arrestin and G protein interactions with GPCRs: a structural perspectiveChapter 6 - GPCRs at endosomes: sorting, signaling, and recyclingChapter 7 - Post-translational Control of GPCR SignalingChapter 8 - GPCR Signaling from Intracellular MembranesChapter 9 - Ten years of GPCR structuresChapter 10 - Activation of class B GPCR by peptide ligands: general structural aspectsChapter 11 - Dynamical basis of GPCR-G-protein coupling selectivity and promiscuityChapter 12 - Virtual Screening and Bioactivity Modeling for G Protein-Coupled ReceptorsChapter 13 - Importance of structure and dynamics in the rational drug design ofG protein-coupled receptor (GPCR) modulatorsChapter 14 - Signaling, Physiology and Targeting of GPCR-Regulated Phospholipase C EnzymesChapter 15 - G Protein-coupled Receptors in Metabolic DiseaseChapter 16 - Endothelin Receptors in cerebrovascular diseasesChapter 17 - The calcium-sensing receptor (CaSR) in diseaseChapter 18 - G protein-coupled receptors and their mutations in cancer - a focus on adenosine receptorsChapter 19 - Dopamine Receptors: Neurotherapeutic Targets for Substance Use DisordersChapter 20 - PTHR1 in boneChapter 21 - Activators of G-protein Signaling in the normal and diseased kidneyChapter 22 - Screening and characterization of GPCR-ligand interactions with mass spectrometry-based technologiesChapter 23 - Bioluminescence resonance energy transfer (BRET) technologies to study GPCRsChapter 24 - The Application of 19F NMR to Studies of Protein Function and Drug ScreeningChapter 25 - Chapter X: Optical Approaches for Dissecting GPCR SignalingChapter 26 - GPCR Signaling in Nanodomains: Lessons from Single-Molecule Microscopy