Inhibition of cell-surface neutral protease of Ehrlich ascites tumor cells by potassium p-(3,3-dimethyl-1-triazeno) benzoate.
Ehrlich ascites tumour (EAT) cells possess a trypsin-like neutral protease on the cell surface. The antimetastatic triazene drug potassium p-(3,3-dimethyl-1-triazeno) benzoate (DM-COOK) inhibits this neutral protease, and also trypsin. Incubation of EAT cells with human erythrocytes (ratio of 1 to 5) at 37 degrees C for 18 h caused haemolysis of 28.8% of the erythrocytes. Addition of millimolar concentrations of DM-COOK to a fixed quantity (2.5 X 10(8)) of EAT cells caused a dose-related inhibition of haemolysis. DM-COOK was strongly bound to EAT cells and could not be removed by repeated washing.
D000626:Aminopeptidases / Q000037:antagonists & inhibitors; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D002286:Carcinoma, Ehrlich Tumor / Q000201:enzymology*; D056655:Cathepsin H; D002403:Cathepsins; D002462:Cell Membrane / Q000201:enzymology; D003546:Cysteine Endopeptidases; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D051379:Mice; D009362:Neoplasm Metastasis; D015260:Neprilysin; D011480:Protease Inhibitors; D014226:Triazenes / Q000494:pharmacology*; D014361:Trypsin Inhibitors
D000970:Antineoplastic Agents; D011480:Protease Inhibitors; D014226:Triazenes; D014361:Trypsin Inhibitors; C030838:1-(4-carboxyphenyl)-3,3-dimethyltriazene; D002403:Cathepsins; D000626:Aminopeptidases; D003546:Cysteine Endopeptidases; C534126:CTSH protein, human; D056655:Cathepsin H; C534127:Ctsh protein, mouse; D015260:Neprilysin