Steven F S, Griffin M M, Williams L A, Ali H, Maier H
Department of Biochemistry and Molecular Biology, School of Biological Sciences, University of Manchester, U.K.
Anticancer Res. 1989 Jan-Feb;9(1):247-53.
Actively migrating tumour cells possess the proteolytic enzyme guanidinobenzoatase (GB) in an uninhibited form. This enzyme has been used as a target for the delivery of adriamycin to invasive tumour cells in frozen sections. An adriamycin-agmatine complex has been prepared which act as a competitive inhibitor of GB. Competition experiments have demonstrated that the adriamycin-agmatine complex competes with 9-aminoacridine for the active centre of GB associated with invasive tumour cells, located in the lymph nodes and in squamous cell carcinoma of the oral cavity. The technique described should be generally applicable to the targeting of drugs to cells.
正在积极迁移的肿瘤细胞拥有未受抑制形式的蛋白水解酶胍基苯甲酸酶（GB）。这种酶已被用作将阿霉素递送至冰冻切片中侵袭性肿瘤细胞的靶点。已经制备了一种阿霉素-胍丁胺复合物，它作为GB的竞争性抑制剂。竞争实验表明，阿霉素-胍丁胺复合物与9-氨基吖啶竞争与侵袭性肿瘤细胞相关的GB活性中心，这些侵袭性肿瘤细胞位于淋巴结和口腔鳞状细胞癌中。所描述的技术应普遍适用于将药物靶向细胞。
