Biased signaling in class A GPCRs
Biased signaling enables selective G protein–coupled receptor (GPCR) pathway modulation with reduced side effects, offering a promising strategy for structure guided drug development.
Structural insights into GPCR conformations have laid the foundation for structure-based drug design, enabling the rational development of ligands that selectively modulate biased signaling pathways.’
Combining cryo–electron microscopy with functional assays provides complementary structural and functional insights into GPCR biased signaling.
Early structural elucidation of receptor ligand complexes can polish mechanistic hypotheses and accelerate biased GPCR drug development.
https://www.cell.com/trends/pharmacological-sciences/fulltext/S0165-6147(25)00232-9
