Direct coupling of detergent purified human mGlu5 receptor to the heterotrimeric G proteins Gq and Gs.

ABSTRACT: The metabotropic glutamate (mGlu) receptors are class C G protein-coupled receptors (GPCRs) that modulate synaptic activity and plasticity throughout the mammalian brain. Signal transduction is initiated by glutamate binding to the venus flytrap domains (VFT), which initiates a conformational change that is transmitted to the conserved heptahelical domains (7TM) and results ultimately in the activation of intracellular G proteins. While both mGlu1 and mGlu5 activate Gαq G-proteins, they also increase intracellular cAMP concentration through an unknown mechanism. To study directly the G protein coupling properties of the human mGlu5 receptor homodimer, we purified the full-length receptor, which required careful optimisation of the expression, N-glycosylation and purification. We successful

SUBMITTER: Nasrallah C 

PROVIDER: S-EPMC5849714 | biostudies-literature | 2018 Mar

REPOSITORIES: biostudies-literature