G-protein-coupled receptors (GPCRs) are the largest class
of signaling receptors that are most frequently targeted
by therapeutic drugs.
Allosteric modulators bound to GPCRs at allosteric sites
provide the potential for differential selectivity and
improved safety compared with traditional orthosteric ligands.
The recent breakthroughs in GPCR structural biology have made
structures of GPCRs from classes A, B, C, and F complexed with
small-molecule allosteric modulators available.
Knowledge of the detailed receptor–modulator interactions
at the allosteric sites is useful for structure-based
GPCR drug design of novel therapeutics.
This Perspective comprehensively summarizes the current status of structural complexes between GPCRs and their small-molecule allosteric modulators, particularly the key receptor–modulator interactions at the allosteric sites.
Then, the structural diversity of allosteric sites across four GPCR subfamilies is compared.
This study is expected to contribute to the design of GPCR allosteric drugs with an improved therapeutic action.
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