As one of the most successful therapeutic target families, G protein-coupled receptors (GPCRs) have experienced a transformation from random ligand screening to knowledge-driven drug design. We are eye-witnessing tremendous progresses made recently in the understanding of their structure-function relationships that facilitated drug development at an unprecedented pace. This article intends to provide a comprehensive overview of this important field to a broader readership that shares some common interests in drug discovery.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7790836PMC
http://dx.doi.org/10.1038/s41392-020-00435-wDOI Listing

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