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PDBsum entry 3fas
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Membrane protein
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PDB id
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3fas
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References listed in PDB file
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Key reference
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Title
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Molecular mechanism of agonist recognition by the ligand-Binding core of the ionotropic glutamate receptor 4.
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Authors
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C.Kasper,
K.Frydenvang,
P.Naur,
M.Gajhede,
D.S.Pickering,
J.S.Kastrup.
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Ref.
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Febs Lett, 2008,
582,
4089-4094.
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PubMed id
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Abstract
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The alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) class of
ionotropic glutamate receptors comprises four different subunits: iGluR1/iGluR2
and iGluR3/iGluR4 forming two subgroups. Three-dimensional structures have been
reported only of the ligand-binding core of iGluR2. Here, we present two X-ray
structures of a soluble construct of the R/G unedited flip splice variant of the
ligand-binding core of iGluR4 (iGluR4(i)(R)-S1S2) in complex with glutamate or
AMPA. Subtle, but important differences are found in the ligand-binding cavity
between the two AMPA receptor subgroups at position 724 (Tyr in iGluR1/iGluR2
and Phe in iGluR3/iGluR4), which in iGluR4 may lead to displacement of a water
molecule and hence points to the possibility to make subgroup specific ligands.
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