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PDBsum entry 2p2a
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Membrane protein
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PDB id
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2p2a
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Contents |
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* Residue conservation analysis
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PDB id:
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Membrane protein
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Title:
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X-ray structure of the glur2 ligand binding core (s1s2j) in complex with 2-bn-tet-ampa at 2.26a resolution
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Structure:
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Glutamate receptor 2. Chain: a, b. Fragment: glur2-flop ligand-binding core (residues 413-527, 653-796). Synonym: glur-2, glur-b, glur-k2, glutamate receptor ionotropic, ampa 2, ampa-selective glutamate receptor 2. Engineered: yes
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Source:
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Rattus norvegicus. Norway rat. Organism_taxid: 10116. Gene: gria2. Expressed in: escherichia coli bl21(de3). Expression_system_taxid: 469008.
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Resolution:
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2.26Å
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R-factor:
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0.211
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R-free:
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0.273
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Authors:
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K.Frydenvang,J.S.Kastrup,M.Gajhede
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Key ref:
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S.B.Vogensen
et al.
(2007).
A tetrazolyl-substituted subtype-selective AMPA receptor agonist.
J Med Chem,
50,
2408-2414.
PubMed id:
DOI:
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Date:
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07-Mar-07
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Release date:
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19-Jun-07
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PROCHECK
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Headers
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References
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P19491
(GRIA2_RAT) -
Glutamate receptor 2 from Rattus norvegicus
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Seq:
Struc:
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883 a.a.
258 a.a.*
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Key: |
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PfamA domain |
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Secondary structure |
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CATH domain |
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*
PDB and UniProt seqs differ
at 2 residue positions (black
crosses)
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DOI no:
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J Med Chem
50:2408-2414
(2007)
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PubMed id:
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A tetrazolyl-substituted subtype-selective AMPA receptor agonist.
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S.B.Vogensen,
K.Frydenvang,
J.R.Greenwood,
G.Postorino,
B.Nielsen,
D.S.Pickering,
B.Ebert,
U.Bølcho,
J.Egebjerg,
M.Gajhede,
J.S.Kastrup,
T.N.Johansen,
R.P.Clausen,
P.Krogsgaard-Larsen.
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ABSTRACT
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Replacement of the methyl group of the AMPA receptor agonist
2-amino-3-[3-hydroxy-5-(2-methyl-2H-5-tetrazolyl)-4-isoxazolyl]propionic acid
(2-Me-Tet-AMPA) with a benzyl group provided the first AMPA receptor agonist,
compound 7, capable of discriminating GluR2-4 from GluR1 by its more than
10-fold preference for the former receptor subtypes. An X-ray crystallographic
analysis of this new analogue in complex with the GluR2-S1S2J construct shows
that accommodation of the benzyl group creates a previously unobserved pocket in
the receptor, which may explain the remarkable pharmacological profile of
compound 7.
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Literature references that cite this PDB file's key reference
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PubMed id
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Reference
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J.Pøhlsgaard,
K.Frydenvang,
U.Madsen,
and
J.S.Kastrup
(2011).
Lessons from more than 80 structures of the GluA2 ligand-binding domain in complex with agonists, antagonists and allosteric modulators.
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Neuropharmacology,
60,
135-150.
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R.Risgaard,
K.B.Hansen,
and
R.P.Clausen
(2010).
Partial agonists and subunit selectivity at NMDA receptors.
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Chemistry,
16,
13910-13918.
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J.K.Nelson,
B.Twamley,
T.J.Villalobos,
and
N.R.Natale
(2008).
The catalytic asymmetric addition of alkyl- and aryl-zinc reagents to an isoxazole aldehyde.
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Tetrahedron Lett,
49,
5957-5960.
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The most recent references are shown first.
Citation data come partly from CiteXplore and partly
from an automated harvesting procedure. Note that this is likely to be
only a partial list as not all journals are covered by
either method. However, we are continually building up the citation data
so more and more references will be included with time.
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Links
