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Insights into Receptor Function and New Drug Development Targets
G-Protein Coupled receptors (GPCRs) and other receptors are significant targets for drug discovery, due to their roles in fundamental physiological processes. Among these roles are: regulation of growth, food intake, reproduction, water balance, sensory perception, blood pressure and heart rate. GPCR-directed drugs account for approximately $40 billion in sales and, of drugs at market, approximately 70% target GPCR function. The availability of combinatorial chemistry coupled with high throughput screening techniques have facilitated discovery of peptidic and non-peptidic ligands of membrane receptors. Mutant receptor models have revealed their role in health and disease and provided insight to new therapeutic approaches, based on control of protein trafficking. Understanding receptor-receptor interactions has provided one mechanism for receptor cross-talk and revealed unexpected interactions.
GPCRs as Therapeutic Targets ; 2-Vol. Set
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.
GPCRs : From Deorphanization to Lead Structure Identification
The book highlights the following topics: Structure of GPCRs, Design of GPCR Ligands, GPCR Signalling, Deorphanization and Assay Development. All chapters are written by leading experts in the field, discussing the most recent state of the art. They give insight into the approaches taken by industry and academia to address GPCRs and depict how mature this target class-oriented research has become in the last decade. The book reflects the actual trends in the fast-emerging field of GPCR research in academia and industry.
Drug discovery and GBCR – Related CNS Disorders
Neurodegenerative diseases are a large group of neurological disorders with diverse etiological and pathological phenomena. However, current therapeutics rely mostly on symptomatic relief while failing to target the underlying disease pathobiology. G-protein-coupled receptors (GPCRs) are one of the most frequently targeted receptors for developing novel therapeutics for central nervous system (CNS) disorders. Many currently available antipsychotic therapeutics also act as either antagonists or agonists of different GPCRs. Therefore, GPCR-based drug development is spreading widely to regulate neurodegeneration and associated cognitive deficits through the modulation of canonical and noncanonical signals.
Chemokines and Viral Infection
This edition of Current Topics in Microbiology and Immunology examines the role of chemokines and chemokine receptors in host defense and disease development following viral infection. Chemokines represent a family of over 40 small proteins that, for the most part, are secreted into the environment and function by binding to G protein-coupled receptors (GPCRs) that are expressed on numerous different cell types. When initially identified close to 30 years ago, these molecules were associated with various human inflammatory diseases and it was recognized that expression may be integral in leukocyte recruitment to inflamed tissue. There are now four sub-families of chemokines identified based on defined structural criteria relating to the positional location of conserved cysteine residues within the amino-terminus of the protein. Chemokines are now recognized as important in numerous biological processes ranging from maintaining the organizational integrity of secondary lymphoid tissue to participating in various aspects of both innate and adaptive immune responses following microbial infection. With this in mind, this book highlights the functional roles of chemokines and their receptors in participating in various aspects of the immune response against well-known viral pathogens.
