The ability of structurally distinct ligands to “bias” G protein-coupled receptor signaling affords the opportunity to tailor efficacy to suit specific therapeutic needs. Furness et al. demonstrate that ligand structure controls not only which effectors are activated, but also the way they are activated and the kinetics of downstream signaling.
Luttrell, L. M. (2016, October 20). GPCR Signaling Rides a Wave of Conformational Changes. Cell. Cell Press. https://doi.org/10.1016/j.cell.2016.10.006