Steven F S, Griffin M M, Barnett F B, Epenetos A A
Department of Biochemistry and Molecular Biology, School of Biological Sciences, University of Manchester, UK.
J Enzyme Inhib. 1990;4(1):63-73. doi: 10.3109/14756369009030390.
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.
肿瘤细胞表面蛋白酶的活性中心可通过其对活性位点导向抑制剂9-氨基吖啶的亲和力来定位。具有未受抑制蛋白酶的细胞会结合9-氨基吖啶，并在树脂切片中发出荧光。白血病大鼠被用作模型系统，以在明确的位置提供肿瘤细胞。当药物与一种配体（导向蛋白酶的活性中心）偶联时，会与9-氨基吖啶竞争这个结合位点。因此，对肿瘤细胞表面蛋白酶的竞争性抑制提供了一种快速技术，用于在体外证明配体化分子递送至肿瘤细胞表面。
