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PDBsum entry 1nnp

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protein ligands Protein-protein interface(s) links
Membrane protein PDB id
1nnp
Jmol
Contents
Protein chains
258 a.a. *
Ligands
SO4 ×2
CE2 ×2
Waters ×725
* Residue conservation analysis
PDB id:
1nnp
Name: Membrane protein
Title: X-ray structure of the glur2 ligand-binding core (s1s2j) in complex with (s)-atpa at 1.9 a resolution. Crystallization without zinc ions.
Structure: Glutamate receptor 2. Chain: a, b. Fragment: glur2-flop ligand-binding core (s1s2j). Synonym: glur-2, glur-b, glur-k2, glutamate receptor ionotropic ampa 2. Engineered: yes
Source: Rattus norvegicus. Norway rat. Organism_taxid: 10116. Expressed in: escherichia coli bl21(de3). Expression_system_taxid: 469008.
Biol. unit: Dimer (from PQS)
Resolution:
1.90Å     R-factor:   0.190     R-free:   0.216
Authors: M.L.Lunn,A.Hogner,T.B.Stensbol,E.Gouaux,J.Egebjerg, J.S.Kastrup
Key ref: M.L.Lunn et al. (2003). Three-dimensional structure of the ligand-binding core of GluR2 in complex with the agonist (S)-ATPA: implications for receptor subunit selectivity. J Med Chem, 46, 872-875. PubMed id: 12593667 DOI: 10.1021/jm021020+
Date:
14-Jan-03     Release date:   11-Mar-03    
PROCHECK
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 Headers
 References

Protein chains
Pfam   ArchSchema ?
P19491  (GRIA2_RAT) -  Glutamate receptor 2
Seq:
Struc:
 
Seq:
Struc:
883 a.a.
258 a.a.*
Key:    PfamA domain  PfamB domain  Secondary structure  CATH domain
* PDB and UniProt seqs differ at 2 residue positions (black crosses)

 Gene Ontology (GO) functional annotation 
  GO annot!
  Cellular component     membrane   1 term 
  Biological process     transport   1 term 
  Biochemical function     transporter activity     3 terms  

 

 
DOI no: 10.1021/jm021020+ J Med Chem 46:872-875 (2003)
PubMed id: 12593667  
 
 
Three-dimensional structure of the ligand-binding core of GluR2 in complex with the agonist (S)-ATPA: implications for receptor subunit selectivity.
M.L.Lunn, A.Hogner, T.B.Stensbøl, E.Gouaux, J.Egebjerg, J.S.Kastrup.
 
  ABSTRACT  
 
Two X-ray structures of the GluR2 ligand-binding core in complex with (S)-2-amino-3-(5-tert-butyl-3-hydroxy-4-isoxazolyl)propionic acid ((S)-ATPA) have been determined with and without Zn(2+) ions. (S)-ATPA induces a domain closure of ca. 21 degrees compared to the apo form. The tert-butyl moiety of (S)-ATPA is buried in a partially hydrophobic pocket and forces the ligand into the glutamate-like binding mode. The structures provide new insight into the molecular basis of agonist selectivity between AMPA and kainate receptors.
 

Literature references that cite this PDB file's key reference

  PubMed id Reference
22948927 S.S.Cha, Y.J.An, C.S.Jeong, M.K.Kim, S.G.Lee, K.H.Lee, and B.H.Oh (2012).
Experimental phasing using zinc anomalous scattering.
  Acta Crystallogr D Biol Crystallogr, 68, 1253-1258.
PDB codes: 4dt3 4dwz 4fc5
20713069 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.
  Neuropharmacology, 60, 135-150.  
16892196 D.Catarzi, V.Colotta, and F.Varano (2007).
Competitive AMPA receptor antagonists.
  Med Res Rev, 27, 239-278.  
16474411 P.E.Chen, and D.J.Wyllie (2006).
Pharmacological insights obtained from structure-function studies of ionotropic glutamate receptors.
  Br J Pharmacol, 147, 839-853.  
15794751 B.B.Nielsen, D.S.Pickering, J.R.Greenwood, L.Brehm, M.Gajhede, A.Schousboe, and J.S.Kastrup (2005).
Exploring the GluR2 ligand-binding core in complex with the bicyclical AMPA analogue (S)-4-AHCP.
  FEBS J, 272, 1639-1648.
PDB code: 1wvj
15677325 M.H.Nanao, T.Green, Y.Stern-Bach, S.F.Heinemann, and S.Choe (2005).
Structure of the kainate receptor subunit GluR6 agonist-binding domain complexed with domoic acid.
  Proc Natl Acad Sci U S A, 102, 1708-1713.
PDB code: 1yae
15919192 M.L.Mayer (2005).
Glutamate receptor ion channels.
  Curr Opin Neurobiol, 15, 282-288.  
16099829 M.M.Holm, M.L.Lunn, S.F.Traynelis, J.S.Kastrup, and J.Egebjerg (2005).
Structural determinants of agonist-specific kinetics at the ionotropic glutamate receptor 2.
  Proc Natl Acad Sci U S A, 102, 12053-12058.  
15224382 K.Strømgaard, and I.Mellor (2004).
AMPA receptor ligands: synthetic and pharmacological studies of polyamines and polyamine toxins.
  Med Res Rev, 24, 589-620.  
15236343 L.Brehm, J.R.Greenwood, F.A.Sløk, M.M.Holm, B.Nielsen, U.Geneser, T.B.Stensbøl, H.Bräuner-Osborne, M.Begtrup, J.Egebjerg, and P.Krogsgaard-Larsen (2004).
Synthesis, theoretical and structural analyses, and enantiopharmacology of 3-carboxy homologs of AMPA.
  Chirality, 16, 452-466.  
15229875 M.Kubo, and E.Ito (2004).
Structural dynamics of an ionotropic glutamate receptor.
  Proteins, 56, 411-419.  
14977400 M.L.Mayer, and N.Armstrong (2004).
Structure and function of glutamate receptor ion channels.
  Annu Rev Physiol, 66, 161-181.  
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. Where a reference describes a PDB structure, the PDB codes are shown on the right.