1wvj
From Proteopedia
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|PDB= 1wvj |SIZE=350|CAPTION= <scene name='initialview01'>1wvj</scene>, resolution 1.75Å | |PDB= 1wvj |SIZE=350|CAPTION= <scene name='initialview01'>1wvj</scene>, resolution 1.75Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= <scene name='pdbligand= | + | |LIGAND= <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=IBC:3-(3-HYDROXY-7,8-DIHYDRO-6H-CYCLOHEPTA[D]ISOXAZOL-4-YL)-L-ALANINE'>IBC</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene> |
|ACTIVITY= | |ACTIVITY= | ||
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY=[[1ftj|1FTJ]], [[1ftm|1FTM]], [[1m5b|1M5B]] | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1wvj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1wvj OCA], [http://www.ebi.ac.uk/pdbsum/1wvj PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1wvj RCSB]</span> | ||
}} | }} | ||
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[[Category: Pickering, D S.]] | [[Category: Pickering, D S.]] | ||
[[Category: Schousboe, A.]] | [[Category: Schousboe, A.]] | ||
| - | [[Category: GOL]] | ||
| - | [[Category: IBC]] | ||
| - | [[Category: SO4]] | ||
[[Category: complex with bicyclic ampa analogue]] | [[Category: complex with bicyclic ampa analogue]] | ||
[[Category: ionotropic glutamate receptor glur2]] | [[Category: ionotropic glutamate receptor glur2]] | ||
[[Category: ligand-binding core]] | [[Category: ligand-binding core]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:41:35 2008'' |
Revision as of 21:41, 30 March 2008
| |||||||
| , resolution 1.75Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , , | ||||||
| Related: | 1FTJ, 1FTM, 1M5B
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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
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