Dual optical control and mechanistic insights into photoswitchable group II and III metabotropic glutamate receptors.

ABSTRACT: G protein-coupled receptor (GPCR) signaling occurs in complex spatiotemporal patterns that are difficult to probe using standard pharmacological and genetic approaches. A powerful approach for dissecting GPCRs is to use light-controlled pharmacological agents that are tethered covalently and specifically to genetically engineered receptors. However, deficits in our understanding of the mechanism of such photoswitches have limited application of this approach and its extension to other GPCRs. In this study, we have harnessed the power of bioorthogonal tethering to SNAP and CLIP protein tags to create a family of light-gated metabotropic glutamate receptors (mGluRs). We define the mechanistic determinants of photoswitch efficacy, including labeling efficiency, dependence on photoswitch struc

SUBMITTER: Levitz J 

PROVIDER: S-EPMC5410775 | biostudies-literature | 2017 Apr

REPOSITORIES: biostudies-literature