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Structure Report for: 3VJL

Name|Crystal structure of human dipeptidyl peptidase IV (DPP-4) in complex with a prolylthiazolidine inhibitor 2
Revelation date|24-Oct-2012
Family|DPP4N_Peptidase_S9: there are 829 genes in this family, 182 structure(s)
PDB File|ESTHER: header of PDB entry RCSB: Full entry
Akahoshi, F., Kishida, H., Miyaguchi, I., Yoshida, T., Ishii, S.
Ligand|Inhibitor: CHEMBL2147710 Ligand in structure: Ligplot


    Title: Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-y lcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
    Yoshida T, Akahoshi F, Sakashita H, Kitajima H, Nakamura M, Sonda S, Takeuchi M, Tanaka Y, Ueda N and Hayashi Y <20 more author(s)>
    Ref: Bioorganic & Medicinal Chemistry, 20:5705, 2012 : PubMed


    Title: Fused bicyclic heteroarylpiperazine-substituted L-prolylthiazolidines as highly potent DPP-4 inhibitors lacking the electrophilic nitrile group
    Yoshida T, Akahoshi F, Sakashita H, Sonda S, Takeuchi M, Tanaka Y, Nabeno M, Kishida H, Miyaguchi I, Hayashi Y
    Ref: Bioorganic & Medicinal Chemistry, 20:5033, 2012 : PubMed


    Title: [(S)-gamma-(4-Aryl-1-piperazinyl)-l-prolyl]thiazolidines as a novel series of highly potent and long-lasting DPP-IV inhibitors
    Yoshida T, Sakashita H, Akahoshi F, Hayashi Y
    Ref: Bioorganic & Medicinal Chemistry Lett, 17:2618, 2007 : PubMed


    Title: [(S)-gamma-(Arylamino)prolyl]thiazolidine compounds as a novel series of potent and stable DPP-IV inhibitors
    Sakashita H, Akahoshi F, Kitajima H, Tsutsumiuchi R, Hayashi Y
    Ref: Bioorganic & Medicinal Chemistry, 14:3662, 2006 : PubMed


Representative scheme of DPP4N_Peptidase_S9 structure and an image from PDBsum server

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PDB-Sum3VJL Previously Class, Architecture, Topology and Homologous superfamily - PDB-Sum server
FSSP3VJL Fold classification based on Structure-Structure alignment of Proteins - FSSP server
SCOP3VJL Structural Classification Of Protein - SCOP server
PROTEOPEDIA3vjl 3D, interactive encyclopedia of proteins - PROTEOPEDIA server

Send your questions or comments to :
Mail to: Nicolas Lenfant, Thierry Hotelier, Yves Bourne, Pascale Marchot and Arnaud Chatonnet.
Please cite: Lenfant 2013 Nucleic.Acids.Res. or Marchot Chatonnet 2012 Prot.Pept Lett.
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