title: Competitive inhibition of a tumour cell surface protease. A rapid technique for in vitro testing of selective targeting systems.
abstract: The active centre of a protease on the surface of tumour cells can be located by its affinity for an active site-directed inhibitor, 9-amino acridine. Cells which have uninhibited proteases, bind 9-amino acridine and fluoresce in resin sections. The leukaemic rat was used as a model system to provide tumour cells in a well defined location. Drugs when coupled to a ligand (directed to the active centre of the protease) compete for this binding site with 9-amino acridine. Thus, competitive inhibition of the tumour cell surface protease provides a rapid technique for demonstrating the delivery of liganded molecules to the surface of tumour cells in vitro.
authors.affiliation: Department of Biochemistry and Molecular Biology, School of Biological Sciences, University of Manchester, UK.
authors.forename: F S
authors.initials: FS
authors.lastname: Steven
authors.forename: M M
authors.initials: MM
authors.lastname: Griffin
authors.forename: F B
authors.initials: FB
authors.lastname: Barnett
authors.forename: A A
authors.initials: AA
authors.lastname: Epenetos
mesh_terms: D000376:Agmatine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000627:therapeutic use; D000585:Aminacrine / Q000378:metabolism*; D000818:Animals; D001665:Binding Sites; D001667:Binding, Competitive; D014408:Biomarkers, Tumor / Q000032:analysis*; D002265:Carboxylic Ester Hydrolases / Q000032:analysis / Q000037:antagonists & inhibitors; D002462:Cell Membrane / Q000201:enzymology*; D004337:Drug Carriers; D010450:Endopeptidases / Q000032:analysis*; D007680:Kidney Neoplasms / Q000188:drug therapy / Q000201:enzymology* / Q000473:pathology; D007942:Leukemia, Experimental / Q000188:drug therapy / Q000201:enzymology* / Q000473:pathology; D015459:Leukemia-Lymphoma, Adult T-Cell / Q000188:drug therapy / Q000201:enzymology / Q000473:pathology; D016685:Mitomycin; D008937:Mitomycins / Q000138:chemical synthesis / Q000627:therapeutic use*; D011480:Protease Inhibitors / Q000378:metabolism*; D051381:Rats; D013386:Succinates / Q000138:chemical synthesis / Q000627:therapeutic use*
chemical_list: D014408:Biomarkers, Tumor; D004337:Drug Carriers; C068976:MMC complex; D008937:Mitomycins; D011480:Protease Inhibitors; D013386:Succinates; D016685:Mitomycin; D000376:Agmatine; D000585:Aminacrine; D002265:Carboxylic Ester Hydrolases; C037288:guanidinobenzoate esterase; D010450:Endopeptidases