2VIP

Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator

Summary for 2VIP

Entry DOI	10.2210/pdb2vip/pdb
Related	1C5W 1C5X 1C5Y 1C5Z 1EJN 1F5L 1F92 1FV9 1GI7 1GI8 1GI9 1GJ7 1GJ8 1GJ9 1GJA 1GJB 1GJC 1GJD 1KDU 1LMW 1O3P 1O5A 1O5B 1O5C 1OWD 1OWE 1OWH 1OWI 1OWJ 1OWK 1SC8 1SQA 1SQO 1SQT 1U6Q 1VJ9 1VJA 1W0Z 1W10 1W11 1W12 1W13 1W14 2JDE 2VIN 2VIO 2VIQ 2VIV 2VIW
Descriptor	UROKINASE-TYPE PLASMINOGEN ACTIVATOR CHAIN B, ACETATE ION, SULFATE ION, ... (5 entities in total)
Functional Keywords	plasminogen activation, egf-like domain, blood coagulation, inhibitor, polymorphism, glycoprotein, fibrinolysis, kringle, zymogen, secreted, protease, hydrolase, urokinase-type plasminogen activator, pharmaceutical, serine protease, phosphorylation
Biological source	HOMO SAPIENS (HUMAN)
Cellular location	Secreted: P00749
Total number of polymer chains	1
Total formula weight	28982.72
Authors	Frederickson, 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, Last modification date: 2017-07-05)
Primary citation	Frederickson, 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 Cited by PubMed: 18163548 DOI: 10.1021/JM701359Z PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (1.72 Å)

Structure validation