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PDBsum entry 3pd9
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Membrane protein
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PDB id
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3pd9
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References listed in PDB file
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Key reference
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Title
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Biostructural and pharmacological studies of bicyclic analogues of the 3-Isoxazolol glutamate receptor agonist ibotenic acid.
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Authors
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K.Frydenvang,
D.S.Pickering,
J.R.Greenwood,
N.Krogsgaard-Larsen,
L.Brehm,
B.Nielsen,
S.B.Vogensen,
H.Hald,
J.S.Kastrup,
P.Krogsgaard-Larsen,
R.P.Clausen.
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Ref.
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J Med Chem, 2010,
53,
8354-8361.
[DOI no: ]
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PubMed id
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Abstract
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No abstract given.
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Secondary reference #1
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Title
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Three-Dimensional structure of the ligand-Binding core of glur2 in complex with the agonist (s)-Atpa: implications for receptor subunit selectivity.
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Authors
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M.L.Lunn,
A.Hogner,
T.B.Stensbøl,
E.Gouaux,
J.Egebjerg,
J.S.Kastrup.
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Ref.
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J Med Chem, 2003,
46,
872-875.
[DOI no: ]
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PubMed id
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Secondary reference #2
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Title
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Mechanisms for activation and antagonism of an ampa-Sensitive glutamate receptor: crystal structures of the glur2 ligand binding core.
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Authors
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N.Armstrong,
E.Gouaux.
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Ref.
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Neuron, 2000,
28,
165-181.
[DOI no: ]
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PubMed id
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Figure 1.
Figure 1. Ligand Binding Constants for S1S2J(A) Domain
structure of iGluRs showing the S1 and S2 segments in turquoise
and pink, respectively. “Cut” and “link” denote the
edges of the S1S2 construct.(B) K[D] for ^3H-AMPA binding was
24.8 ± 1.8 nM.(C) IC[50] for displacement of ^3H-AMPA by
glutamate, kainate, and DNQX were 821 nM, 14.5 μM, and 998 nM,
respectively.
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Figure 2.
Figure 2. Superposition of the Expanded Cleft Structures and
Stereo View of the DNQX Binding Site(A) The two apo molecules
(ApoA and ApoB) and two DNQX molecules (DNQXA and DNQXB) in each
asymmetric unit were superimposed using only Cα atoms from
domain 1. Apo protomers are shaded red and pink while DNQX
protomers are colored light green and dark green. DNQX is
depicted in black, and selected side chains from DNQXB are shown
in dark green. The conformational change undergone by Glu-705 is
illustrated by comparing its orientation in ApoB and DNQXB. In
the apo state, Glu-705 accepts hydrogen bonds from the side
chains of Lys-730 and Thr-655.(B) The chemical structure of DNQX
and F[o]-F[c] omit electron density for DNQX and sulfate
contoured at 2.5 σ.(C) Stereo image of the interactions between
DNQX, sulfate, and S1S2J. DNQXB side chains are colored gray.
Water molecules are shown as green balls. DNQX is colored black.
Hydrogen bonds between DNQX, sulfate, and S1S2J are indicated by
black dashed lines.
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The above figures are
reproduced from the cited reference
with permission from Cell Press
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