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TitleDesign and Synthesis of a Series of l-trans-4-Substituted Prolines as Selective Antagonists for the Ionotropic Glutamate Receptors Including Functional and X-ray Crystallographic Studies of New Subtype Selective Kainic Acid Receptor Subtype 1 (GluK1) Antagonist (2S,4R)-4-(2-Carboxyphenoxy)pyrrolidine-2-carboxylic Acid.
Journal, issue, pagesJ. Med. Chem., Vol. 60, Page 441-457, Year 2017
Publish dateOct 13, 2016 (structure data deposition date)
AuthorsKrogsgaard-Larsen, N. / Delgar, C.G. / Koch, K. / Brown, P.M. / Moller, C. / Han, L. / Huynh, T.H. / Hansen, S.W. / Nielsen, B. / Bowie, D. ...Krogsgaard-Larsen, N. / Delgar, C.G. / Koch, K. / Brown, P.M. / Moller, C. / Han, L. / Huynh, T.H. / Hansen, S.W. / Nielsen, B. / Bowie, D. / Pickering, D.S. / Kastrup, J.S. / Frydenvang, K. / Bunch, L.
External linksJ. Med. Chem. / PubMed:28005385
MethodsX-ray diffraction
Resolution3.18 Å
Structure data

PDB-5m2v:
Structure of GluK1 ligand-binding domain (S1S2) in complex with (2S,4R)-4-(2-carboxyphenoxy)pyrrolidine-2-carboxylic acid at 3.18 A resolution
Method: X-RAY DIFFRACTION / Resolution: 3.18 Å

Chemicals

ChemComp-7E5:
(2~{S},4~{R})-4-(2-carboxyphenoxy)pyrrolidine-2-carboxylic acid

ChemComp-SO4:
SULFATE ION

ChemComp-CL:
Unknown entry

Source
  • rattus norvegicus (Norway rat)
KeywordsMEMBRANE PROTEIN / Kainate receptor ligand-binding domain / GluK1-LBD / GluK1-S1S2 / antagonist

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