Structure of a Class C GPCR Metabotropic Glutamate Receptor 1 Bound to an Allosteric Modulator-Reference-Cited by-同舟云学术

Structure of a Class C GPCR Metabotropic Glutamate Receptor 1 Bound to an Allosteric Modulator

Published:2014-04-04 Issue:6179 Volume:344 Page:58-64
ISSN:0036-8075
Container-title:Science
language:en
Short-container-title:Science

Author:

Wu Huixian¹,Wang Chong¹,Gregory Karen J.²³,Han Gye Won¹,Cho Hyekyung P.²,Xia Yan⁴,Niswender Colleen M.²,Katritch Vsevolod¹,Meiler Jens⁴,Cherezov Vadim¹,Conn P. Jeffrey²,Stevens Raymond C.¹

Affiliation:

1. Department of Integrative Structural and Computational Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.

2. Department of Pharmacology and Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA.

3. Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia.

4. Center for Structural Biology and Department of Chemistry and Institute for Chemical Biology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.

Abstract

Completing the Set G protein–coupled receptors (GPCRs) are membrane proteins that transduce extracellular signals to activate diverse signaling pathways. Significant insight into GPCR function has come from structures of three of four classes of GPCRs—A, B, and Frizzled. Wu et al. (p. 58 , published online 6 March) complete the picture by reporting the structure of metabotropic glutamate receptor 1, a class C GPCR. The structure shows differences in the seven-transmembrane (7TM) domain between class C and other classes; however, the overall fold is preserved. Class C GPCRs are known to form dimers through their extracellular domains; however, the structure suggests additional interactions between the 7TM domains mediated by cholesterol.

Publisher

American Association for the Advancement of Science (AAAS)

Subject

Multidisciplinary

Reference68 articles.

1. Structural diversity of G protein-coupled receptors and significance for drug discovery

2. Dimers and beyond: The functional puzzles of class C GPCRs

3. Structures of the extracellular regions of the group II/III metabotropic glutamate receptors

4. Cloning, Expression, and Gene Structure of a G Protein-Coupled Glutamate Receptor from Rat Brain

5. Sequence and expression of a metabotropic glutamate receptor

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