Competitive inhibition of a tumour cell surface protease. A rapid technique for in vitro testing of selective targeting systems |
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Authors: | F S Steven M M Griffin F B Barnett A A Epenetos |
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Affiliation: | Department of Biochemistry and Molecular Biology, School of Biological Sciences, University of Manchester, UK. |
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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. |
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