2p2a: Difference between revisions

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[[Image:2p2a.jpg|left|200px]]
{{Seed}}
[[Image:2p2a.png|left|200px]]


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{{STRUCTURE_2p2a|  PDB=2p2a  |  SCENE=  }}  
{{STRUCTURE_2p2a|  PDB=2p2a  |  SCENE=  }}  


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




==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.
The line below this paragraph, {{ABSTRACT_PUBMED_17455929}}, adds the Publication Abstract to the page
(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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