2cmo

File:2cmo.gif

spinqualitylabelsall models 2cmo, resolution 2.65Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

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

OverviewOverview

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 StructureAbout 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].

ReferenceReference

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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