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The G protein-coupled receptor (GPCR) family is among the most druggable families in the human proteome. GPCRs are involved in most physiological processes, and our ability to modulate their activity is a hallmark of modern pharmacology. The means by which the activity of GPCRs can be modulated have been expanded by emerging data and concepts in pharmacology, which has created new strategies for their control. These new approaches will lead to the generation of more potent, selective, anddoi:10.1016/j.ceb.2013.11.006 pmid:24680430 pmcid:PMC3971376 fatcat:mn3c4gy53famdn2bnqwwuemz6i