A tool to study the dynamic process of receptor activation

G protein-coupled receptors (GPCRs), the largest family of membrane proteins, enable cells to respond to a wide array of extracellular stimuli and control diverse intracellular signaling pathways. The Class C GPCRs, which contain the metabotropic glutamate receptors (mGluRs) and GABAB receptors, are expressed throughout the nervous system where they control excitability and synaptic strength and serve as drug targets for many neurological disorders including schizophrenia, fragile x syndrome, Alzheimer’s disease and depression. Understanding how Class C GPCRs are activated may aid the development of drugs for the treatment of these neurological disorders. GPCRs change their shape when an activating ligand binds. Specific conformational changes activate the receptor and trigger intracellular signaling. To understand this dynamic process, Reza Vafabakhsh and Joshua Levitz from Ehud Isacoff’s Lab developed a novel single-molecule fluorescence…


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