Thursday, April 3, 2014
Publication and contact
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.
All contents Copyright © 1993-2015 BioCentury Publications, Inc. ALL RIGHTS RESERVED. All use of this Web Site and its contents is governed by the BioCentury User Agreement
. The contents of this Web Site are protected under U.S. and foreign copyright and intellectual property laws, and no part of this Web Site or its contents may be photocopied, reproduced or retransmitted in any form without the written consent of BioCentury, which may be requested from Reprints/Permissions
. BioCentury®; The Bernstein Report on BioBusiness™; The BioCentury 100™; The Clear Route to ROI™; Because Real Intelligence is Hard to Find™; BCIQ™; and BioPharma's Knowledge Center™; are trademarks of BioCentury Publications, Inc., P.O. Box 1246, San Carlos, CA 94070. SciBX® and SciBX: Science-Business eXchange® are trademarks of Nature America, Inc. that are jointly used by BioCentury Publications, Inc. and Nature America, Inc.
Thanks for purchasing this article.
Please bookmark this url for future reference.
We have also sent you a confirming e-mail with a receipt and this same url for your
close [ X ]