The endothelin subtype A receptor undergoes agonist- and antagonist-mediated internalization in the absence of signaling.

摘要: The potent vasoconstrictor and mitogen to smooth muscle cells, endothelin-1 (ET-1), acts via two distinct G protein-coupled receptors, subtype A (ETAR) B, that are coupled primarily the Gq-phospholipase C signaling pathway. It is known ET-1 binding ETAR promotes internalization, with subsequent degradation of at least a portion bound ligand. To investigate whether required for endocytosis, we developed stably transfected lines human embryonic kidney 293 cells expressing wild-type receptor chimera (ETARC) in which C-terminal cytoplasmic tail was replaced lutropin receptor, another but one signals through Gs-adenylyl cyclase ETARC binds like ETAR, deficient signaling. Using combined concanavalin A/sucrose gradient centrifugation technique separate plasma membranes from other cellular membranes, found [125I]ET-1 rapidly internalized into ETAR-expr...