1wvj
From Proteopedia
| Line 1: | Line 1: | ||
[[Image:1wvj.gif|left|200px]] | [[Image:1wvj.gif|left|200px]] | ||
| - | + | <!-- | |
| - | + | The line below this paragraph, containing "STRUCTURE_1wvj", creates the "Structure Box" on the page. | |
| - | + | You may change the PDB parameter (which sets the PDB file loaded into the applet) | |
| - | + | or the SCENE parameter (which sets the initial scene displayed when the page is loaded), | |
| - | | | + | or leave the SCENE parameter empty for the default display. |
| - | | | + | --> |
| - | + | {{STRUCTURE_1wvj| PDB=1wvj | SCENE= }} | |
| - | + | ||
| - | + | ||
| - | }} | + | |
'''Exploring the GluR2 ligand-binding core in complex with the bicyclic AMPA analogue (S)-4-AHCP''' | '''Exploring the GluR2 ligand-binding core in complex with the bicyclic AMPA analogue (S)-4-AHCP''' | ||
| Line 32: | Line 29: | ||
[[Category: Pickering, D S.]] | [[Category: Pickering, D S.]] | ||
[[Category: Schousboe, A.]] | [[Category: Schousboe, A.]] | ||
| - | [[Category: | + | [[Category: Complex with bicyclic ampa analogue]] |
| - | [[Category: | + | [[Category: Ionotropic glutamate receptor glur2]] |
| - | [[Category: | + | [[Category: Ligand-binding core]] |
| - | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 14:11:45 2008'' | |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | |
Revision as of 11:11, 3 May 2008
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. 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 Page seeded by OCA on Sat May 3 14:11:45 2008
