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. 1991 Jan 31;174(2):779-84.
doi: 10.1016/0006-291x(91)91485-u.

Phosphoramidon inhibits the intracellular conversion of big endothelin-1 to endothelin-1 in cultured endothelial cells

T Sawamura  1 , Y Kasuya, Y Matsushita, N Suzuki, O Shinmi, N Kishi, Y Sugita, M Yanagisawa, K Goto, T Masaki, et al.
Affiliations

Phosphoramidon inhibits the intracellular conversion of big endothelin-1 to endothelin-1 in cultured endothelial cells

T Sawamura et al. Biochem Biophys Res Commun. .

Abstract

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.

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