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New Binding Sites, New Opportunities for GPCR Drug Discovery

Author:
Chan, H.C. Stephen, Li, Yi, Dahoun, Thamani, Vogel, Horst, Yuan, Shuguang
Source:
Trends in biochemical sciences 2019 v.44 no.4 pp. 312-330
ISSN:
0968-0004
Subject:
G-protein coupled receptors, G-proteins, binding sites, drugs, ligands, protein binding
Abstract:
Many central biological events rely on protein–ligand interactions. The identification and characterization of protein-binding sites for ligands are crucial for the understanding of functions of both endogenous ligands and synthetic drug molecules. G protein-coupled receptors (GPCRs) typically detect extracellular signal molecules on the cell surface and transfer these chemical signals across the membrane, inducing downstream cellular responses via G proteins or β-arrestin. GPCRs mediate many central physiological processes, making them important targets for modern drug discovery. Here, we focus on the most recent breakthroughs in finding new binding sites and binding modes of GPCRs and their potentials for the development of new medicines.
Agid:
6252156