2p2a: Difference between revisions

Revision as of 12:11, 4 May 2008

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

OverviewOverview

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.

About this StructureAbout this Structure

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

ReferenceReference

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 Page seeded by OCA on Sun May 4 12:11:19 2008

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA

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 [[Image:2p2a.jpg|left|200px]]
- {{Structure
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-|GENE= Gria2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Rattus norvegicus])
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-|DOMAIN=
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-|RELATEDENTRY=[[1ftj|1FTJ]], [[1ftm|1FTM]], [[1m5b|1M5B]]
-|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2p2a FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2p2a OCA], [http://www.ebi.ac.uk/pdbsum/2p2a PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2p2a RCSB]</span>
-}}
 '''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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 [[Category: Gajhede, M.]]
 [[Category: Kastrup, J S.]]
-[[Category: agonist complex]]
+[[Category: Agonist complex]]
-[[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 Sun May  4 12:11:19 2008''
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:27:33 2008''