G-Protein-coupled receptor oligomerization and its potential for drug discovery

By S. George, B. O'dowd, Samuel P. Lee. Nature reviews. Drug discovery, 2002

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GLIDA: GPCR-ligand database for chemical genomic drug discovery (2005, background): “These molecules regulate various cellular functions responsible for physiological responses (1).”
Subcellular targeting strategies for drug design and delivery (2010, background): “Owing to their involvement in many disease processes, GPCRs are important drug target”
Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders (2009, background): “jpg" NDATA ITEM> ]> G-protein-coupled receptors (GPCRs) are the largest class of cell-surface receptors and play crucial roles in virtually every organ system (see Ref”
Heterotrimeric G protein activation by G-protein-coupled receptors (2008, background): “Heterodimerization may result in signalling complexes that have unique ligand binding and G protein coupling properties compared with the component receptor”
Roles of G‐protein‐coupled receptor dimerization (2004, background): “In particular, it could provide new opportunities for the development of more selective compounds that would target specific heterodimers without affecting the individual protomers (George et al, 2002).”