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.
journal_name
J Pharmacol Scijournal_title
Journal of pharmacological sciencesauthors
Horinouchi T,Karki S,Terada K,Mazaki Y,Miwa Sdoi
10.1016/j.jphs.2019.03.008subject
Has Abstractpub_date
2019-05-01 00:00:00pages
102-105issue
1eissn
1347-8613issn
1347-8648pii
S1347-8613(19)31047-3journal_volume
140pub_type
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