FitzGerald D, Pastan I
Laboratory of Molecular Biology, National Cancer Institute, Bethesda, MD 20892.
Semin Cell Biol. 1991 Feb;2(1):31-7.
Pseudomonas exotoxin (PE) is a three-domain bacterial toxin that kills mammalian cells by gaining entry to the cytosol and inactivating protein synthesis. The pathway of toxin entry includes binding to a surface receptor, internalization via coated pits and endosomes, proteolytic processing, reduction of disulfide bonds and finally the translocation of an enzymatically active C-terminal fragment to the cytosol. Once in the cytosol this fragment inhibits protein synthesis by ADP ribosylating elongation factor 2. Because of its potency PE and its derivatives have been directed to kill various target cells. It is hoped this strategy will lead to the development of a novel kind of therapeutic agent for the treatment of various human diseases including cancer, AIDS and various immunological disorders.
铜绿假单胞菌外毒素（PE）是一种三结构域细菌毒素，它通过进入细胞质溶胶并使蛋白质合成失活来杀死哺乳动物细胞。毒素进入的途径包括与表面受体结合、通过被膜小窝和内体进行内化、蛋白水解加工、二硫键还原，最终将具有酶活性的C末端片段转运到细胞质溶胶中。一旦进入细胞质溶胶，该片段通过对延伸因子2进行ADP核糖基化来抑制蛋白质合成。由于其效力，PE及其衍生物已被用于杀死各种靶细胞。人们希望这种策略将导致开发出一种新型治疗剂，用于治疗包括癌症、艾滋病和各种免疫紊乱在内的各种人类疾病。
