Journal
DRUG DISCOVERY TODAY
Volume 26, Issue 3, Pages 690-703Publisher
ELSEVIER SCI LTD
DOI: 10.1016/j.drudis.2020.12.001
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Funding
- National Natural Science Foundation of China [22077082, 21778037, 91753117, 81721004]
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As a superfamily of membrane receptors, G-protein-coupled receptors (GPCRs) have significant roles in human physiological processes, including cell proliferation, metabolism, and neuromodulation. GPCRs are vital targets of therapeutic drugs, and their allosteric regulation represents a novel direction for drug discovery. Given the numerous breakthroughs in structural biology, diverse allosteric sites on GPCRs have been identified within the extracellular and intracellular loops, and the seven core transmembrane helices. However, a unique type of allosteric site has also been discovered at the interface of the receptor-lipid bilayer, similar to the beta(2)-adrenergic receptor. Here, we review recent identifications of these allosteric sites and the detailed modulator-target interactions within the interface for each modulator to highlight the role of lipids in GPCR allosteric drug discovery.
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