{Reference Type}: Journal Article
{Title}: Ca2+ signal is involved in endothelin-1-induced internalization of endothelin type A receptor expressed in Chinese hamster ovary cells.
{Author}: Horinouchi T;Karki S;Terada K;Mazaki Y;Miwa S;
{Journal}: J Pharmacol Sci
{Volume}: 140
{Issue}: 1
{Year}: May 2019
{Factor}: 3.578
{DOI}: 10.1016/j.jphs.2019.03.008
{Abstract}: Endothelin type A receptor (ETAR) is internalized upon agonist stimulation; however, the mechanism thereof remains controversial. In this study, we characterized the endothelin-1 (ET-1)-induced internalization of ETAR expressed in Chinese hamster ovary cells. ET-1 elicited ETAR internalization and increase in intracellular Ca2+ concentration. ET-1-induced ETAR internalization was completely inhibited by a reduction in intracellular and extracellular Ca2+ levels and partially suppressed by inhibitors of protein kinase C (PKC) and extracellular signal-regulated kinases 1/2 (ERK1/2), both of which are downstream molecules in ETAR signaling. These results suggest that Ca2+ mobilization, PKC, and ERK1/2 are involved in ET-1-induced ETAR internalization.