Competitive inhibition of a tumour cell surface protease. A rapid technique for in vitro testing of selective targeting systems

Journal of Enzyme Inhibition
F S StevenA A Epenetos

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.

References

Jul 1, 1975·Pathology·M DibleyB Roser
Jan 1, 1988·Journal of Enzyme Inhibition·F S StevenM Altmannsberger
Jan 1, 1986·Journal of Enzyme Inhibition·F S StevenS Itzhaki
Jun 15, 1986·International Journal of Cancer. Journal International Du Cancer·F S StevenN C Jackson
Nov 1, 1984·British Journal of Cancer·H JacksonM Lendon
Feb 1, 1983·The Biochemical Journal·S P LeytusW F Mangel
May 6, 1983·Science·D J HnatowichP W Doherty

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