PHOSPHORAMIDON INHIBITS THE INTRACELLULAR CONVERSION OF BIG ENDOTHELIN-1 TO ENDOTHELIN-1 IN CULTURED ENDOTHELIAL-CELLS

被引:91
作者
SAWAMURA, T
KASUYA, Y
MATSUSHITA, Y
SUZUKI, N
SHINMI, O
KISHI, N
SUGITA, Y
YANAGISAWA, M
GOTO, K
MASAKI, T
KIMURA, S
机构
[1] UNIV TSUKUBA,INST BASIC MED SCI,DEPT BIOCHEM,TSUKUBA,IBARAKI 305,JAPAN
[2] TAKEDA CHEM IND LTD,TSUKUBA RES LABS,TSUKUBA,IBARAKI 30042,JAPAN
[3] UNIV TSUKUBA,INST BASIC MED SCI,DEPT PHARMACOL,TSUKUBA,IBARAKI 305,JAPAN
关键词
D O I
10.1016/0006-291X(91)91485-U
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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 increases 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. © 1991.
引用
收藏
页码:779 / 784
页数:6
相关论文
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