Journal
NATURE
Volume 559, Issue 7712, Pages 45-53Publisher
NATURE PUBLISHING GROUP
DOI: 10.1038/s41586-018-0259-z
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Funding
- National Health and Medical Research Council of Australia (NHMRC) [APP1055134]
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G-protein-coupled receptors (GPCRs) are key cell-surface proteins that transduce external environmental cues into biochemical signals across the membrane. GPCRs are intrinsically allosteric proteins; they interact via spatially distinct yet conformationally linked domains with both endogenous and exogenous proteins, nutrients, metabolites, hormones, small molecules and biological agents. Here we explore recent high-resolution structural studies, which are beginning to unravel the atomic details of allosteric transitions that govern GPCR biology, as well as highlighting how the wide diversity of druggable allosteric sites across these receptors present opportunities for developing new classes of therapeutics.
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