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1p1n

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{{STRUCTURE_1p1n| PDB=1p1n | SCENE= }}
{{STRUCTURE_1p1n| PDB=1p1n | SCENE= }}
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'''GluR2 Ligand Binding Core (S1S2J) Mutant L650T in Complex with Kainate'''
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===GluR2 Ligand Binding Core (S1S2J) Mutant L650T in Complex with Kainate===
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==Overview==
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The (S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazole) propionic acid (AMPA) receptor discriminates between agonists in terms of binding and channel gating; AMPA is a high-affinity full agonist, whereas kainate is a low-affinity partial agonist. Although there is extensive literature on the functional characterization of partial agonist activity in ion channels, structure-based mechanisms are scarce. Here we investigate the role of Leu-650, a binding cleft residue conserved among AMPA receptors, in maintaining agonist specificity and regulating agonist binding and channel gating by using physiological, x-ray crystallographic, and biochemical techniques. Changing Leu-650 to Thr yields a receptor that responds more potently and efficaciously to kainate and less potently and efficaciously to AMPA relative to the WT receptor. Crystal structures of the Leu-650 to Thr mutant reveal an increase in domain closure in the kainate-bound state and a partially closed and a fully closed conformation in the AMPA-bound form. Our results indicate that agonists can induce a range of conformations in the GluR2 ligand-binding core and that domain closure is directly correlated to channel activation. The partially closed, AMPA-bound conformation of the L650T mutant likely captures the structure of an agonist-bound, inactive state of the receptor. Together with previously solved structures, we have determined a mechanism of agonist binding and subsequent conformational rearrangements.
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{{ABSTRACT_PUBMED_12730367}}
==About this Structure==
==About this Structure==
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[[Category: Mayer, M L.]]
[[Category: Mayer, M L.]]
[[Category: Ionotropic glutamate receptor]]
[[Category: Ionotropic glutamate receptor]]
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Revision as of 17:19, 28 July 2008

Image:1p1n.png

Template:STRUCTURE 1p1n

GluR2 Ligand Binding Core (S1S2J) Mutant L650T in Complex with Kainate

Template:ABSTRACT PUBMED 12730367

About this Structure

1P1N is a Single protein structure of sequence from Rattus norvegicus. Full crystallographic information is available from OCA.

Reference

Tuning activation of the AMPA-sensitive GluR2 ion channel by genetic adjustment of agonist-induced conformational changes., Armstrong N, Mayer M, Gouaux E, Proc Natl Acad Sci U S A. 2003 May 13;100(10):5736-41. Epub 2003 May 2. PMID:12730367

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