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Review Sep 2026

The promise of biased ligands in therapeutics.

Discovered 40 years ago but underappreciated for decades, the paradigm of biased agonism has now become standard in G protein-coupled receptor (GPCR) pharmacology and drug discovery. Biased agonism refers to the phenomenon in which different agonists binding to the same receptor result in differential activation of sig...

D. Eiger, Jeffrey S. Smith, S. Rajagopal · 0 citations
Open access Sep 2026

Identifying common G protein–coupled receptor interacting proteins independent of heterotrimeric G proteins and β-arrestins

Abstract The canonical paradigm of G protein–coupled receptor (GPCR) signaling recognizes G proteins, β-arrestins, and GPCR kinases as the primary transducers that shape GPCR signaling. However, multiple studies have demonstrated that other interacting proteins regulate GPCR function in addition to these pathways, term...

Chloe Hicks, Julia Gardner, Anand Chundi et al. · 0 citations

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