Steven F S, Griffin M M, Wong T L, Jackson H, Barnett F
Department of Biochemistry, University of Manchester, UK.
J Enzyme Inhib. 1987;1(3):203-13. doi: 10.3109/14756368709020117.
Guanidinobenzoatase is a trypsin-like protease on the surface of cells capable of migration, for example leukaemia cells. We have used a number of fluorescent probes that are competitive inhibitors of guanidinobenzoatase to locate leukaemia cells in resin sections of kidney tissue obtained from leukaemic rats. We have demonstrated how this competitive inhibition system can be used to direct desired molecules (such as cytotoxic drugs) to these cells and to monitor the arrival of such compounds at the active site of guanidinobenzoatase. The principles developed in this study could equally well be applied to other enzymes on other cells provided suitable competitive inhibitors were designed. The presence of an enzyme on the surface of a cell can be used to direct molecules to that cell provided that these molecules contain a functional group that acts as an inhibitor for the chosen enzyme.
胍基苯甲酸酶是一种存在于能够迁移的细胞表面的类胰蛋白酶，例如白血病细胞。我们使用了多种作为胍基苯甲酸酶竞争性抑制剂的荧光探针，来在从白血病大鼠获取的肾组织树脂切片中定位白血病细胞。我们已经证明了这种竞争性抑制系统可如何用于将所需分子（如细胞毒性药物）导向这些细胞，并监测此类化合物到达胍基苯甲酸酶活性位点的情况。只要设计出合适的竞争性抑制剂，本研究中所开发的原理同样可应用于其他细胞上的其他酶。细胞表面存在的一种酶可用于将分子导向该细胞，前提是这些分子含有一个作为所选酶抑制剂的官能团。
