Thursday, April 3, 2014
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Crystal structure of metabotropic
glutamate receptor subtype 1 (mGluR1;
The crystal structure of
mGluR1 could help researchers design mGluR1-targeted therapeutics to treat
cancer and various neurological indications. In vitro, an X-ray
crystal structure of the dimeric, seven-transmembrane domain of mGluR1 bound
to a negative allosteric modulator revealed that the overall fold of the
transmembrane domain and the modulator binding site resembled the inactive
conformation of other classes of G protein-coupled receptors. In this
structure, six cholesterols mediated contact between dimerizing receptor
subunits, suggesting cholesterol could mediate communication between the
extracellular domain that initiates dimerization and the transmembrane
domain. Next steps include understanding allosteric mechanisms governing
receptor activity and using the structure to optimize allosteric modulators.
Published online April 3, 2014
status not applicable
Wu, H. et al. Science;
published online March 6, 2014;
Contact: Raymond C. Stevens, The Scripps Research Institute,
La Jolla, Calif.
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