DEFINITION
Biased agonism (also called functional selectivity) describes the phenomenon in which two agonists at the same receptor engage its downstream signalling arms — for example G-protein coupling versus β-arrestin recruitment — in different proportions.
At GLP-1R and other class B GPCRs, biased agonism is an active research area with potential implications for separating desired pharmacology from receptor desensitisation and internalisation. The clinical significance of ligand bias at GLP-1R for existing agonists such as Semaglutide is not yet fully mapped.
WHY IT MATTERS
Biased agonism is a foundational conceptual framework for interpreting differences between GLP-1 receptor agonists at the signalling level.
RELATED
Compounds