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 diseases
Perfect 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.
Table of Contents
Chapter 1 - An overview of G protein coupled receptors and their signaling partners
Chapter 2 - Recent advances in orphan GPCRs research and therapeutic potential
Chapter 3 - The Evolution of Our Understanding of GPCRs
Chapter 4 - Approaching GPCR dimers and higher order oligomers using biophysical, biochemical and proteomic methods
Chapter 5 - Arrestin and G protein interactions with GPCRs: a structural perspective
Chapter 6 - GPCRs at endosomes: sorting, signaling, and recycling
Chapter 7 - Post-translational Control of GPCR Signaling
Chapter 8 - GPCR Signaling from Intracellular Membranes
Chapter 9 - Ten years of GPCR structures
Chapter 10 - Activation of class B GPCR by peptide ligands: general structural aspects
Chapter 11 - Dynamical basis of GPCR-G-protein coupling selectivity and promiscuity
Chapter 12 - Virtual Screening and Bioactivity Modeling for G Protein‐Coupled Receptors
Chapter 13 - Importance of structure and dynamics in the rational drug design of
G protein-coupled receptor (GPCR) modulators
Chapter 14 - Signaling, Physiology and Targeting of GPCR-Regulated Phospholipase C Enzymes
Chapter 15 - G Protein-coupled Receptors in Metabolic Disease
Chapter 16 - Endothelin Receptors in cerebrovascular diseases
Chapter 17 - The calcium-sensing receptor (CaSR) in disease
Chapter 18 - G protein-coupled receptors and their mutations in cancer - a focus on adenosine receptors
Chapter 19 - Dopamine Receptors: Neurotherapeutic Targets for Substance Use Disorders
Chapter 20 - PTHR1 in bone
Chapter 21 - Activators of G-protein Signaling in the normal and diseased kidney
Chapter 22 - Screening and characterization of GPCR-ligand interactions with mass spectrometry-based technologies
Chapter 23 - Bioluminescence resonance energy transfer (BRET) technologies to study GPCRs
Chapter 24 - The Application of 19F NMR to Studies of Protein Function and Drug Screening
Chapter 25 - Chapter X: Optical Approaches for Dissecting GPCR Signaling
Chapter 26 - GPCR Signaling in Nanodomains: Lessons from Single-Molecule Microscopy
