Sawamura T, Kasuya Y, Matsushita Y, Suzuki N, Shinmi O, Kishi N, Sugita Y, Yanagisawa M, Goto K, Masaki T
Department of Biochemistry, University of Tsukuba, Ibaraki, Japan.
Biochem Biophys Res Commun. 1991 Jan 31;174(2):779-84. doi: 10.1016/0006-291x(91)91485-u.
Effects of various protease inhibitors on the conversion of big endothelin (ET)-1 to ET-1 in cultured endothelial cells were analyzed. A metal protease inhibitor, phosphoramidon, decreases the amount of ET-1 and increase that of big ET-1 released. This effect is dose-dependent and not nonspecific. When the contents of ET-1 and big ET-1 in the cells after culturing in the medium with or without phosphoramidon were measured, the ratio of ET-1: big ET-1 in the cells was 3.3 : 1 and phosphoramidon inverted the ratio in the cells to 1 : 3.5. These data strongly suggest that a phosphoramidon-sensitive protease converts big ET-1 to mature ET-1 intracellularly.
分析了各种蛋白酶抑制剂对培养的内皮细胞中大内皮素（ET）-1向ET-1转化的影响。一种金属蛋白酶抑制剂磷酰胺素，可减少ET-1的量并增加释放的大ET-1的量。这种作用具有剂量依赖性，并非非特异性的。当测量在含或不含磷酰胺素的培养基中培养后细胞内ET-1和大ET-1的含量时，细胞中ET-1与大ET-1的比例为3.3:1，而磷酰胺素将细胞中的比例颠倒为1:3.5。这些数据有力地表明，一种对磷酰胺素敏感的蛋白酶在细胞内将大ET-1转化为成熟的ET-1。
