Skip to main content

Biased Agonism

Meaning

Biased agonism, also known as functional selectivity, describes a phenomenon where a ligand binding to a G protein-coupled receptor (GPCR) selectively activates one intracellular signaling pathway over others. Unlike traditional agonists that activate all downstream pathways equally, a biased agonist preferentially steers the receptor toward a specific physiological response. This nuanced activation profile is critical in pharmacology, allowing for the design of targeted therapeutics with reduced side-effect profiles. Understanding this concept is key to developing precision endocrine modulators.