3b7d

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spinqualitylabelsall models 3b7d, resolution 2.50Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

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 with as ligand. 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 Wed Jan 23 12:11:35 2008