Article
Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator.
Science (New York, N.Y.) - 4 Apr 2014
Wu Huixian, Wang Chong, Gregory Karen J, Han Gye Won, Cho Hyekyung P, Xia Yan, Niswender Colleen M, Katritch Vsevolod, Meiler Jens, Cherezov Vadim, Conn P Jeffrey, Stevens Raymond C
Abstract excerpt
The excitatory neurotransmitter glutamate induces modulatory actions via the metabotropic glutamate receptors (mGlus), which are class C G protein-coupled receptors (GPCRs). We determined the structure of the human mGlu1 receptor seven-transmembrane (7TM) domain bound to a negative allosteric modulator, FITM, at a resolution of 2.8 angstroms. The modulator binding site partially overlaps with the orthosteric...
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