Signaling Rides a Wave of Conformational Changes

Description

Commentary on:

Furness SGB, Liang YL, Nowell CJ, Halls ML, Wookey PJ, Dal Maso E, Inoue A, Christopoulos A, Wootten D, Sexton PM. Ligand-Dependent Modulation of G Protein Conformation Alters Drug Efficacy. Cell. 2016 Oct 20;167(3):739-749.e11. doi: 10.1016/j.cell.2016.09.021. Epub 2016 Oct 6. PubMed PMID: 27720449.

 

 

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.