G protein-coupled receptors (GPCR) are a super-family of membrane proteins and major targets for drug development. However, many GPCRs drug candidates suffer from a lack of selectivity. Photopharmacology gives the possibility of modulating GPCR activity with an unprecedented local and temporal precision with the use of light. In this review, we compilate and classify of the different strategies in photopharmacology for GPCRs, we revise the different methods of analysis and characterisation of light-regulated molecules used for GPCRs and we gave perspective of the impact of photopharmacology in research applications and in the development of new drugs.
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