GPCRs as Therapeutic Targets

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 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.

Annette Gilchrist, PhD, is an Associate Professor at Midwestern University in the Department of Pharmaceutical Sciences.

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

The New copy of this book will include any supplemental materials advertised. Please check the title of the book to determine if it should include any access cards, study guides, lab manuals, CDs, etc.

The Used, Rental and eBook copies of this book are not guaranteed to include any supplemental materials. Typically, only the book itself is included. This is true even if the title states it includes any access cards, study guides, lab manuals, CDs, etc.