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1wvj

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[[Image:1wvj.gif|left|200px]]
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{{STRUCTURE_1wvj| PDB=1wvj | SCENE= }}
{{STRUCTURE_1wvj| PDB=1wvj | SCENE= }}
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'''Exploring the GluR2 ligand-binding core in complex with the bicyclic AMPA analogue (S)-4-AHCP'''
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===Exploring the GluR2 ligand-binding core in complex with the bicyclic AMPA analogue (S)-4-AHCP===
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==Overview==
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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.
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The line below this paragraph, {{ABSTRACT_PUBMED_15794751}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 15794751 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15794751}}
==About this Structure==
==About this Structure==
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==Reference==
==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:[http://www.ncbi.nlm.nih.gov/pubmed/15794751 15794751]
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:[http://www.ncbi.nlm.nih.gov/pubmed/15794751 15794751]
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Structural basis for AMPA receptor activation and ligand selectivity: crystal structures of five agonist complexes with the GluR2 ligand-binding core., Hogner A, Kastrup JS, Jin R, Liljefors T, Mayer ML, Egebjerg J, Larsen IK, Gouaux E, J Mol Biol. 2002 Sep 6;322(1):93-109. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12215417 12215417]
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Mechanisms for activation and antagonism of an AMPA-sensitive glutamate receptor: crystal structures of the GluR2 ligand binding core., Armstrong N, Gouaux E, Neuron. 2000 Oct;28(1):165-81. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/11086992 11086992]
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Probing the ligand binding domain of the GluR2 receptor by proteolysis and deletion mutagenesis defines domain boundaries and yields a crystallizable construct., Chen GQ, Sun Y, Jin R, Gouaux E, Protein Sci. 1998 Dec;7(12):2623-30. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/9865957 9865957]
[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: Ionotropic glutamate receptor glur2]]
[[Category: Ionotropic glutamate receptor glur2]]
[[Category: Ligand-binding core]]
[[Category: Ligand-binding core]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 14:11:45 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 19:00:11 2008''

Revision as of 16:00, 27 July 2008

Image:1wvj.png

Template:STRUCTURE 1wvj

Exploring the GluR2 ligand-binding core in complex with the bicyclic AMPA analogue (S)-4-AHCP

Template:ABSTRACT PUBMED 15794751

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

Structural basis for AMPA receptor activation and ligand selectivity: crystal structures of five agonist complexes with the GluR2 ligand-binding core., Hogner A, Kastrup JS, Jin R, Liljefors T, Mayer ML, Egebjerg J, Larsen IK, Gouaux E, J Mol Biol. 2002 Sep 6;322(1):93-109. PMID:12215417

Mechanisms for activation and antagonism of an AMPA-sensitive glutamate receptor: crystal structures of the GluR2 ligand binding core., Armstrong N, Gouaux E, Neuron. 2000 Oct;28(1):165-81. PMID:11086992

Probing the ligand binding domain of the GluR2 receptor by proteolysis and deletion mutagenesis defines domain boundaries and yields a crystallizable construct., Chen GQ, Sun Y, Jin R, Gouaux E, Protein Sci. 1998 Dec;7(12):2623-30. PMID:9865957

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