Optical measurement of mGluR1 conformational changes reveals fast activation, slow deactivation, and sensitization.

ABSTRACT: Metabotropic glutamate receptor (mGluR) activation has been extensively studied under steady-state conditions. However, at central synapses, mGluRs are exposed to brief submillisecond glutamate transients and may not reach steady-state. The lack of information on the kinetics of mGluR activation impairs accurate predictions of their operation during synaptic transmission. Here, we report experiments designed to investigate mGluR kinetics in real-time. We inserted either CFP or YFP into the second intracellular loop of mGluR1beta. When these constructs were coexpressed in PC12 cells, glutamate application induced a conformational change that could be monitored, using fluorescence resonance energy transfer (FRET), with an EC(50) of 7.5 microM. The FRET response was mimicked by the agonist DH

SUBMITTER: Marcaggi P 

PROVIDER: S-EPMC2700146 | biostudies-literature | 2009 Jul

REPOSITORIES: biostudies-literature