Conversion of big endothelin-1 to 21-residue endothelin-1 is essential for expression of full vasoconstrictor activity: Structure-activity relationships of big endothelin-1

S. Kimura, Y. Kasuya, T. Sawamura, O. Shinmi, Y. Sugita, Masashi Yanagisawa, K. Goto, T. Masaki

Research output: Contribution to journalArticle

181 Scopus citations

Abstract

The vasoconstrictor activities of porcine big endothelin-1 (big ET-1), a 39-residue intermediate predicted from cDNA sequence analysis, and of its shorter derivative, big ET-1 [1-25], were characterized in vitro by measuring the contraction of porcine coronary artery strips. Synthetic big ET-1 [1-39] and big ET-1 [1-25] induced a slow developing, long-lasting, and strong vasoconstriction as in the case of 21-residue ET-1. However, the contractile molar potencies of big ET-1 [1-39] and big ET-1 [1-25] were approximately 140-and 50-fold lower than that of ET-1, respectively. These results indicate that the conversion of big ET-1 to "mature" ET-1 is essential for the expression of the full vasoconstrictor activity, suggesting the physiological importance of the unusual proteolytic processing catalyzed by the putative "ET converting enzyme.

Original languageEnglish (US)
Pages (from-to)S5-S7
JournalJournal of Cardiovascular Pharmacology
Volume13
DOIs
StatePublished - 1989

Keywords

  • Big endothelin-1
  • Coronary arteries
  • Endothelial cells
  • Endothelin converting enzyme
  • Endothelin-1
  • Structure-activity relationships

ASJC Scopus subject areas

  • Pharmacology
  • Cardiology and Cardiovascular Medicine

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