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PDBsum entry 2xxi
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Transport protein
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PDB id
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2xxi
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PDB id:
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| Name: |
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Transport protein
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Title:
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Crystal structure of 1-((4-(3-(trifluoromethyl)-6,7-dihydropyrano(4,3- c(pyrazol-1(4h)-yl)phenyl)methyl)-2-pyrrolidinone in complex with the ligand binding domain of the rat glua2 receptor and glutamate at 1.6a resolution.
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Structure:
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Glutamate receptor 2. Chain: a, b, c. Fragment: ligand binding domain, residues 413-527,653-796. Synonym: glur-2, ampa-selective glutamate receptor 2, glur-b, glur- k2, glutamate receptor ionotropic\,ampa 2, glua2. Engineered: yes. Mutation: yes. Other_details: glua2flops1-glythr-s2
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Source:
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Rattus norvegicus. Norway rat. Organism_taxid: 10116. Expressed in: escherichia coli. Expression_system_taxid: 469008.
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Resolution:
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1.60Å
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R-factor:
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0.191
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R-free:
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0.208
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Authors:
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S.E.Ward,M.Harries,L.Aldegheri,N.E.Austin,S.Ballantine,E.Ballini, D.M.Bradley,B.D.Bax,B.P.Clarke,A.J.Harris,S.A.Harrison, R.A.Melarange,C.Mookherjee,J.Mosley,G.Dalnegro,B.Oliosi,K.J.Smith, K.M.Thewlis,P.M.Woollard,S.P.Yusaf
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Key ref:
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S.E.Ward
et al.
(2011).
Integration of lead optimization with crystallography for a membrane-bound ion channel target: discovery of a new class of AMPA receptor positive allosteric modulators.
J Med Chem,
54,
78-94.
PubMed id:
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Date:
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10-Nov-10
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Release date:
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06-Apr-11
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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.
263 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 5 residue positions (black
crosses)
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J Med Chem
54:78-94
(2011)
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PubMed id:
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Integration of lead optimization with crystallography for a membrane-bound ion channel target: discovery of a new class of AMPA receptor positive allosteric modulators.
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S.E.Ward,
M.Harries,
L.Aldegheri,
N.E.Austin,
S.Ballantine,
E.Ballini,
D.M.Bradley,
B.D.Bax,
B.P.Clarke,
A.J.Harris,
S.A.Harrison,
R.A.Melarange,
C.Mookherjee,
J.Mosley,
G.Dal Negro,
B.Oliosi,
K.J.Smith,
K.M.Thewlis,
P.M.Woollard,
S.P.Yusaf.
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ABSTRACT
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Links
