Takai S, Shiota N, Jin D, Miyazaki M
Department of Pharmacology, Osaka Medical College, Takatsuki, Japan.
Eur J Pharmacol. 1998 Oct 9;358(3):229-33. doi: 10.1016/s0014-2999(98)00622-0.
Purified monkey chymase cleaved the Tyr31-Gly32 bond of big-endothelin-1 and big-endothelin-2 to yield endothelin-1-(1-31) and endothelin-2-(1-31), respectively. In the isolated monkey trachea, endothelin-1-(1-31) and endothelin-2-(1-31), as well as big-endothelin-1 and big-endothelin-2, induced contractile responses. Chymostatin, which inhibits chymase, suppressed the contractile response induced by big-endothelin-2 to 16.6% but not the responses induced by big-endothelin-1, endothelin-1-(1-31) and endothelin-2-(1-31). These results suggest that the contractile response of big-endothelin-2 is predominantly dependent on the conversion of big-endothelin-2 to endothelin-2-(1-31) by chymase.
