2p2a

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{{STRUCTURE_2p2a| PDB=2p2a | SCENE= }}
{{STRUCTURE_2p2a| PDB=2p2a | SCENE= }}
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'''X-ray structure of the GluR2 ligand binding core (S1S2J) in complex with 2-Bn-tet-AMPA at 2.26A resolution'''
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===X-ray structure of the GluR2 ligand binding core (S1S2J) in complex with 2-Bn-tet-AMPA at 2.26A resolution===
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==Overview==
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Replacement of the methyl group of the AMPA receptor agonist 2-amino-3-[3-hydroxy-5-(2-methyl-2H-5-tetrazolyl)-4-isoxazolyl]propionic acid (2-Me-Tet-AMPA) with a benzyl group provided the first AMPA receptor agonist, compound 7, capable of discriminating GluR2-4 from GluR1 by its more than 10-fold preference for the former receptor subtypes. An X-ray crystallographic analysis of this new analogue in complex with the GluR2-S1S2J construct shows that accommodation of the benzyl group creates a previously unobserved pocket in the receptor, which may explain the remarkable pharmacological profile of compound 7.
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(as it appears on PubMed at http://www.pubmed.gov), where 17455929 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17455929}}
==About this Structure==
==About this Structure==
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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 Sun May 4 12:11:19 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 12:49:50 2008''

Revision as of 09:49, 29 July 2008

Image:2p2a.png

Template:STRUCTURE 2p2a

X-ray structure of the GluR2 ligand binding core (S1S2J) in complex with 2-Bn-tet-AMPA at 2.26A resolution

Template:ABSTRACT PUBMED 17455929

About this Structure

2P2A is a Single protein structure of sequence from Rattus norvegicus. Full crystallographic information is available from OCA.

Reference

A tetrazolyl-substituted subtype-selective AMPA receptor agonist., Vogensen SB, Frydenvang K, Greenwood JR, Postorino G, Nielsen B, Pickering DS, Ebert B, Bolcho U, Egebjerg J, Gajhede M, Kastrup JS, Johansen TN, Clausen RP, Krogsgaard-Larsen P, J Med Chem. 2007 May 17;50(10):2408-14. Epub 2007 Apr 25. PMID:17455929

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