Tuning up the right signal: chemical and genetic approaches to study GPCR functions

Patrick M Giguere, Wesley K Kroeze, Bryan L Roth
2014 Current Opinion in Cell Biology  
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, and
more » ... ent pharmaceutics, while reducing inappropriate actions and adverse effects. Herein, we review and comment on some recent advances in chemical and genetic approaches to the profiling of GPCR function, as well as the validation of orphan GPCRs as potential therapeutic targets using engineered receptors.
doi:10.1016/j.ceb.2013.11.006 pmid:24680430 pmcid:PMC3971376 fatcat:mn3c4gy53famdn2bnqwwuemz6i