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

SUMMARYThe 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-...

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Veröffentlicht in:Journal of cardiovascular pharmacology 1989, Vol.13 Suppl 5, p.S5-7
Hauptverfasser: Kimura, Sadao, Kasuya, Yoshitoshi, Sawamura, Tatsuya, Shinmi, Osamu, Sugita, Yoshiki, Yanagisawa, Masashi, Goto, Katsutoshi, Masaki, Tomoh
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container_end_page 7
container_issue
container_start_page S5
container_title Journal of cardiovascular pharmacology
container_volume 13 Suppl 5
creator Kimura, Sadao
Kasuya, Yoshitoshi
Sawamura, Tatsuya
Shinmi, Osamu
Sugita, Yoshiki
Yanagisawa, Masashi
Goto, Katsutoshi
Masaki, Tomoh
description SUMMARYThe 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.”
doi_str_mv 10.1097/00005344-198900135-00003
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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. 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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. 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source MEDLINE; Journals@Ovid LWW Legacy Archive; Journals@Ovid Complete; EZB-FREE-00999 freely available EZB journals
subjects Animals
Endothelins
In Vitro Techniques
Muscle Contraction - drug effects
Muscle, Smooth, Vascular - drug effects
Peptides - analysis
Peptides - pharmacology
Structure-Activity Relationship
Swine
Vasoconstriction - drug effects
title 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
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