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β2-adrenoceptor ligand efficacy is tuned by a two-stage interaction with the Gαs C terminus
2021
Proceedings of the National Academy of Sciences of the United States of America
Classical pharmacological models have incorporated an "intrinsic efficacy" parameter to capture system-independent effects of G protein–coupled receptor (GPCR) ligands. However, the nonlinear serial amplification of downstream signaling limits quantitation of ligand intrinsic efficacy. A recent biophysical study has characterized a ligand "molecular efficacy" that quantifies the influence of ligand-dependent receptor conformation on G protein activation. Nonetheless, the structural translation
doi:10.1073/pnas.2017201118
pmid:33836582
fatcat:7mr5dit4gjcb3eeep6q6sjmrii