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. Author manuscript; available in PMC: 2019 Aug 5.
Published in final edited form as: Nat Rev Drug Discov. 2018 Nov 9;18(1):59–82. doi: 10.1038/nrd.2018.180

Figure 1 |. Therapeutic use, efficacy, and biased signaling of GPCR ligands.

Figure 1 |

a | Schematic diagram of GPCR signaling. Activated GPCRs induce signal transduction through independent signaling pathways, either via G proteins or via G protein-coupled receptor kinases (GRKs) and arrestins. b | Schematic diagram of biased signaling. A G protein-biased ligand and an arrestin-biased ligand elicit signaling via the G protein pathway and the arrestin pathway, respectively. c | Examples of clinically effective biased ligands of GPCRs. d | Plots of signaling activity versus ligand concentration, representing different common GPCR efficacies. e | Examples of clinically effective partial agonists of GPCRs.