LigandenBias
LigandenBias is a term used in pharmacology to describe the phenomenon that different ligands binding to the same receptor can produce distinct signaling outcomes. Rather than triggering a uniform response, certain ligands stabilize receptor conformations that preferentially activate specific intracellular pathways, a concept often discussed in the context of G protein-coupled receptors (GPCRs).
Mechanistically, many receptors couple to multiple signaling routes, such as various G proteins (Gs, Gi/o, Gq/11)
Quantification of LigandenBias typically involves comparing ligand activity across several signaling readouts. Models like the Black-Leff
Implications and applications of LigandenBias include the potential to improve therapeutic selectivity and reduce adverse effects