Brand  (β version)

PDB ID: 5OEW

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Ligands
Code Name Style Show Link
GLU Glutamic acid PoSSuM
ZN Zinc ion PoSSuM
ACT Acetate ion PoSSuM
9TE 4-cyclopropyl-7-(3-methoxyphenoxy)-2,3-dihydro-1$L^{6},2,4-benzothiadiazine 1,1-dioxide PoSSuM
Non-standard Residues
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Structure summary

Code : 5OEW   PDBj   RCSB PDB   PDBe
Header : MEMBRANE PROTEIN
Title : Crystal structure of the GluA2 ligand-binding domain (S1S2J) in complex with glutamate and positive allosteric modulator BPAM538
Release Data : 2018-01-03
Compound :
mol_id molecule chains synonym
1 Glutamate receptor 2 A,B,C GluR-2,AMPA-selective glutamate receptor 2,GluR-B,GluR-K2,Glutamate receptor ionotropic,AMPA 2,GluA2
other_details: Ligand-binding domain, UNP residues 413-527 and 653-797 connected by a GT linker (numbering including signal peptide)
Source :
mol_id organism_scientific organism_common expression_system
1 Rattus norvegicus  (taxid:10116) Rat Escherichia coli  (taxid:562)
gene: Gria2, Glur2
Authors : Larsen, A.P., Frydenvang, K.A., Kastrup, J.S.
Keywords : Ionotropic glutamate receptor GluA2. ligand-binding domain, positive allosteric modulator, MEMBRANE PROTEIN
Exp. method : X-RAY DIFFRACTION ( 2.0000 Å )
Citation :

7-Phenoxy-Substituted 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency.

Goffin, E.,Drapier, T.,Larsen, A.P.  et al.
(2018)  J. Med. Chem.  61 : 251 - 264

PubMed: 29256599
DOI: 10.1021/acs.jmedchem.7b01323

Synthesis, pharmacological and structural characterization, and thermodynamic aspects of GluA2-positive allosteric modulators with a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide scaffold.

Norholm, A.B.,Francotte, P.,Olsen, L.  et al.
(2013)  J. Med. Chem.  56 : 8736 - 8745

PubMed: 24131202
DOI: 10.1021/jm4012092

Reaction

Chain : A, B, C
UniProt : P19491 (GRIA2_RAT)
Reaction: EC: Evidence:
Physiological Direction:
Ca(2+)(in) = Ca(2+)(out) - PubMed:11773314, PubMed:1653450
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Na(+)(in) = Na(+)(out) - PubMed:11773314, PubMed:1653450
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