3b7d

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[[Image:3b7d.gif|left|200px]]
[[Image:3b7d.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 3b7d |SIZE=350|CAPTION= <scene name='initialview01'>3b7d</scene>, resolution 2.50&Aring;
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The line below this paragraph, containing "STRUCTURE_3b7d", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=CNI:7-NITRO-2,3-DIOXO-2,3-DIHYDROQUINOXALINE-6-CARBONITRILE'>CNI</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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|GENE= Gria2, Glur2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Rattus norvegicus])
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-->
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|DOMAIN=
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{{STRUCTURE_3b7d| PDB=3b7d | SCENE= }}
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|RELATEDENTRY=[[1ftj|1FTJ]], [[1ftm|1FTM]], [[1fto|1FTO]], [[1ftl|1FTL]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3b7d FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3b7d OCA], [http://www.ebi.ac.uk/pdbsum/3b7d PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=3b7d RCSB]</span>
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}}
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'''Crystal structure of the GLUR2 ligand binding core (HS1S2J) in complex with CNQX at 2.5 A resolution'''
'''Crystal structure of the GLUR2 ligand binding core (HS1S2J) in complex with CNQX at 2.5 A resolution'''
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[[Category: CSMP, Center for Structures of Membrane Proteins.]]
[[Category: CSMP, Center for Structures of Membrane Proteins.]]
[[Category: Hays, F A.]]
[[Category: Hays, F A.]]
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[[Category: alternative splicing]]
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[[Category: Alternative splicing]]
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[[Category: cell junction]]
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[[Category: Cell junction]]
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[[Category: center for structures of membrane protein]]
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[[Category: Center for structures of membrane protein]]
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[[Category: cnqx]]
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[[Category: Cnqx]]
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[[Category: csmp]]
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[[Category: Csmp]]
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[[Category: glycoprotein]]
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[[Category: Glycoprotein]]
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[[Category: Palmitate]]
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[[Category: Phosphorylation]]
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[[Category: postsynaptic cell membrane]]
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[[Category: Postsynaptic cell membrane]]
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[[Category: protein structure initiative]]
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[[Category: Protein structure initiative]]
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[[Category: psi-2]]
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[[Category: Psi-2]]
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[[Category: receptor]]
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[[Category: Receptor]]
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[[Category: rna editing]]
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[[Category: Rna editing]]
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[[Category: s1s2]]
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[[Category: S1s2]]
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[[Category: structural genomic]]
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[[Category: Structural genomic]]
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[[Category: synapse]]
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[[Category: Synapse]]
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[[Category: transmembrane]]
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[[Category: Transmembrane]]
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[[Category: transport]]
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[[Category: Transport]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 20:28:14 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:23:46 2008''
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Revision as of 17:28, 4 May 2008

Image:3b7d.gif

Template:STRUCTURE 3b7d

Crystal structure of the GLUR2 ligand binding core (HS1S2J) in complex with CNQX at 2.5 A resolution


Overview

Quinoxalinedione compounds such as 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) are the most commonly used alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists. However, we find that in the presence of transmembrane AMPA receptor regulatory proteins (TARPs), which are AMPA receptor auxiliary subunits, CNQX acts as a partial agonist. CNQX induced small depolarizing currents in neurons of the central nervous system, and reconstitution of this agonist activity required coexpression of TARPs. A crystal structure of CNQX bound to the TARP-less AMPA receptor ligand-binding domain showed that, although CNQX induces partial domain closure, this movement is not transduced into linker separation, suggesting that TARPs may increase agonist efficacy by strengthening the coupling between domain closure and channel opening. Our results demonstrate that the presence of an auxiliary subunit can determine whether a compound functions as an agonist or antagonist.

About this Structure

3B7D is a Single protein structure of sequence from Rattus norvegicus. Full crystallographic information is available from OCA.

Reference

TARP auxiliary subunits switch AMPA receptor antagonists into partial agonists., Menuz K, Stroud RM, Nicoll RA, Hays FA, Science. 2007 Nov 2;318(5851):815-7. PMID:17975069 Page seeded by OCA on Sun May 4 20:28:14 2008

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