TY - JOUR
T1 - Conversion of big endothelin-1 to 21-residue endothelin-1 is essential for expression of full vasoconstrictor activity
T2 - Structure-activity relationships of big endothelin-1
AU - Kimura, S.
AU - Kasuya, Y.
AU - Sawamura, T.
AU - Shinmi, O.
AU - Sugita, Y.
AU - Yanagisawa, Masashi
AU - Goto, K.
AU - Masaki, T.
PY - 1989
Y1 - 1989
N2 - 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.
AB - 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.
KW - Big endothelin-1
KW - Coronary arteries
KW - Endothelial cells
KW - Endothelin converting enzyme
KW - Endothelin-1
KW - Structure-activity relationships
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U2 - 10.1097/00005344-198900135-00003
DO - 10.1097/00005344-198900135-00003
M3 - Article
C2 - 2473327
AN - SCOPUS:0024521522
SN - 0160-2446
VL - 13
SP - S5-S7
JO - Journal of Cardiovascular Pharmacology
JF - Journal of Cardiovascular Pharmacology
ER -