F1000 recommendation

Description

The work described in this article offers a very interesting new perspective, that is: ligand-induced conformational selection in a G protein-coupled receptor (GPCR) is not limited to the receptor itself, but it also extends to the bound G protein. Specifically, ligand-dependent conformational differences in the G-protein ternary complex appear to control guanine nucleotide exchange, resulting in different accumulation rates for second messengers. This finding was reported in this manuscript for the calcitonin GPCR but it is expected to apply to GPCRs in general, and to eventually shed light on the mechanisms that underlie ligand-induced biased agonism. A molecular-level understanding of how these conformational changes are transmitted throughout the G-protein ternary complex would be highly desirable.

Disclosures

None declared

 

Filizola M: F1000Prime Recommendation of [Furness SGB et al., Cell 2016 167(3):739-749.e11]. In F1000Prime, 18 Oct 2016; 10.3410/f.726827078.793524205