2p2a
From Proteopedia
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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
Overview
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 Structure
2P2A is a Single protein structure of sequence from Rattus norvegicus with , and as ligands. 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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