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PDBsum entry 1pb9
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Ligand binding protein
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PDB id
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1pb9
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Contents |
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* Residue conservation analysis
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References listed in PDB file
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Key reference
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Title
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Mechanisms of activation, Inhibition and specificity: crystal structures of the nmda receptor nr1 ligand-Binding core.
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Authors
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H.Furukawa,
E.Gouaux.
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Ref.
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Embo J, 2003,
22,
2873-2885.
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PubMed id
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Abstract
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Excitatory neurotransmission mediated by the N-methyl-D-aspartate subtype of
ionotropic glutamate receptors is fundamental to the development and function of
the mammalian central nervous system. NMDA receptors require both glycine and
glutamate for activation with NR1 and NR2 forming glycine and glutamate sites,
respectively. Mechanisms to describe agonist and antagonist binding, and
activation and desensitization of NMDA receptors have been hampered by the lack
of high-resolution structures. Here, we describe the cocrystal structures of the
NR1 S1S2 ligand-binding core with the agonists glycine and D-serine (DS), the
partial agonist D-cycloserine (DCS) and the antagonist 5,7-dichlorokynurenic
acid (DCKA). The cleft of the S1S2 'clamshell' is open in the presence of the
antagonist DCKA and closed in the glycine, DS and DCS complexes. In addition,
the NR1 S1S2 structure reveals the fold and interactions of loop 1, a
cysteine-rich region implicated in intersubunit allostery.
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