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Summary Structural Experimental Function Sequence Neighbor Download Link


<Asymmetric unit>
= <Biological unit>

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PDB ID2viq  sequence information (FASTA format)   
RELATED PDB ID1c5w, 1c5x, 1c5y, 1c5z, 1ejn, 1fv9, 1gi7, 1gi9, 1gj7, 1gj8, 1gj9, 1gjc, 1kdu, 1o5c, 1owd, 1owh, 1owj, 1sc8, 1f5l, 1f92, 1gi8, 1gja, 1gjb, 1gjd, 1lmw, 1o3p, 1o5a, 1o5b, 1owe, 1owi, 1owk, 1sqa, 1sqo, 1sqt, 1u6q, 1vj9, 1w0z, 1w10, 1w12, 1w14, 1vja, 1w11, 1w13, 2jde, 2vin, 2vio, 2vip, 2viv, 2viw
DescriptorUROKINASE-TYPE PLASMINOGEN ACTIVATOR CHAIN B (E.C.3.4.21.73)
TitleFRAGMENT-BASED DISCOVERY OF MEXILETINE DERIVATIVES AS ORALLY BIOAVAILABLE INHIBITORS OF UROKINASE-TYPE PLASMINOGEN ACTIVATOR
Functional KeywordsPLASMINOGEN ACTIVATION, EGF-LIKE DOMAIN, BLOOD COAGULATION, INHIBITOR, POLYMORPHISM, GLYCOPROTEIN, FIBRINOLYSIS, KRINGLE, ZYMOGEN, SECRETED, PROTEASE, HYDROLASE, UROKINASE-TYPE PLASMINOGEN ACTIVATOR, PHARMACEUTICAL, SERINE PROTEASE, PHOSPHORYLATION
Biological sourceHOMO SAPIENS (HUMAN)
Cellular location [UNP - P00749] Secreted
Organ source [UNP - P00749] Lung
Total number of polymer chains1
Total molecular weight28876 (the details in Structural Details Page)
AuthorsFrederickson, M. , Callaghan, O. , Chessari, G. , Congreve, M. , Cowan, S.R. , Matthews, J.E. , Mcmenamin, R. , Smith, D. , Vinkovic, M. , Wallis, N.G. (deposition date : 2007-12-05, release date : 2008-01-22)
Primary citationFrederickson, M. , Callaghan, O. , Chessari, G. , Congreve, M. , Cowan, S.R. , Matthews, J.E. , Mcmenamin, R. , Smith, D. , Vinkovic, M. , Wallis, N.G.
Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator.
J.Med.Chem., 51:183 - , 2008.(PubMed : 18163548)  (DOI: 10.1021/jm701359z)
Experimental methodX-RAY DIFFRACTION ( 2.[Å] )
Other Database Information
Yorodumi , CATH , CE , FSSP , SCOP , VAST , UniProt ( P00749 ) , eF-site , KEGG ( EC 3.4.21.73 ) , PISA