1wvj
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(New page: 200px<br /><applet load="1wvj" size="450" color="white" frame="true" align="right" spinBox="true" caption="1wvj, resolution 1.75Å" /> '''Exploring the GluR2 ...)
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Revision as of 22:42, 24 November 2007
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Exploring the GluR2 ligand-binding core in complex with the bicyclic AMPA analogue (S)-4-AHCP
Overview
The X-ray structure of the ionotropic GluR2 ligand-binding core, (GluR2-S1S2J) in complex with the bicyclical AMPA analogue, (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]-4-isoxazolyl)propion, ic acid [(S)-4-AHCP] has been determined, as well as the binding, pharmacology of this construct and of the full-length GluR2 receptor., (S)-4-AHCP binds with a glutamate-like binding mode and the ligand adopts, two different conformations. The K(i) of (S)-4-AHCP at GluR2-S1S2J was, determined to be 185 +/- 29 nM and at full-length GluR2(R)o it was 175 +/-, 8 nM. (S)-4-AHCP appears to elicit partial agonism at GluR2 by inducing an, intermediate degree of domain closure (17 degrees). Also, functionally, (S)-4-AHCP has an efficacy of 0.38 at GluR2(Q)i, relative to, (S)-glutamate. The proximity of bound (S)-4-AHCP to domain D2 prevents, full D1-D2 domain closure, which is limited by steric repulsion, especially between Leu704 and the ligand.
About this Structure
1WVJ is a Single protein structure of sequence from Rattus norvegicus with SO4, IBC and GOL as ligands. Full crystallographic information is available from OCA.
Reference
Exploring the GluR2 ligand-binding core in complex with the bicyclical AMPA analogue (S)-4-AHCP., Nielsen BB, Pickering DS, Greenwood JR, Brehm L, Gajhede M, Schousboe A, Kastrup JS, FEBS J. 2005 Apr;272(7):1639-48. PMID:15794751
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