2cmo

From Proteopedia

Revision as of 11:03, 30 October 2007

THE STRUCTURE OF A MIXED GLUR2 LIGAND-BINDING CORE DIMER IN COMPLEX WITH (S)-GLUTAMATE AND THE ANTAGONIST (S)-NS1209

Overview

Ionotropic glutamate receptors (iGluRs) mediate fast synaptic transmission, between cells of the central nervous system and are involved in various, aspects of normal brain function. iGluRs are implicated in several brain, disorders, e.g. in the high-frequency discharge of impulses during an, epileptic seizure. (RS)-NS1209 functions as a competitive antagonist at, 2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionate receptors, and shows, robust preclinical anticonvulsant and neuroprotective effects. This study, explores 2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionate receptor, binding and selectivity of this novel class of antagonists. We present, here the first X-ray structure of a mixed GluR2 ligand-binding core dimer, with the high-affinity antagonist, ... [(full description)]

About this Structure

2CMO is a [Single protein] structure of sequence from [Rattus norvegicus] with SO4, GLU and M1L as [ligands]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].

Reference

The structure of a mixed GluR2 ligand-binding core dimer in complex with (S)-glutamate and the antagonist (S)-NS1209., Kasper C, Pickering DS, Mirza O, Olsen L, Kristensen AS, Greenwood JR, Liljefors T, Schousboe A, Watjen F, Gajhede M, Sigurskjold BW, Kastrup JS, J Mol Biol. 2006 Apr 7;357(4):1184-201. Epub 2006 Jan 31. PMID:16483599

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