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

Tatsuya Sawamura, Yoshitoshi Kasuya, Yohichi Matsushita, Nobuhiro Suzuki, Osamu Shinmi, Naoya Kishi, Yoshiki Sugita, Masashi Yanagisawa, Katsutoshi Goto, Tomoh Masaki, Sadao Kimura

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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 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.

Original languageEnglish (US)
Pages (from-to)779-784
Number of pages6
JournalBiochemical and Biophysical Research Communications
Volume174
Issue number2
DOIs
StatePublished - Jan 31 1991

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ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

Cite this

Sawamura, T., Kasuya, Y., Matsushita, Y., Suzuki, N., Shinmi, O., Kishi, N., Sugita, Y., Yanagisawa, M., Goto, K., Masaki, T., & Kimura, S. (1991). Phosphoramidon inhibits the intracellular conversion of big endothelin-1 to endothelin-1 in cultured endothelial cells. Biochemical and Biophysical Research Communications, 174(2), 779-784. https://doi.org/10.1016/0006-291X(91)91485-U