Schramek H, Wang Y, Konieczkowski M, Rose P M, Sedor J R, Dunn M J
Department of Medicine, Case Western Reserve University, Cleveland, Ohio 44106.
Biochem Biophys Res Commun. 1994 Mar 15;199(2):992-7. doi: 10.1006/bbrc.1994.1327.
The ability of endothelin-1 (ET-1) to activate cytosolic phospholipase A2 (cPLA2) has been studied in Chinese Hamster ovary (CHO) cells stably expressing either the human ETA (CHO/ETA) or the human ETB (CHO/ETB) receptor subtype. ET-1 dose-dependently increased a dithiothreitol-insensitive cPLA2 activity in both cell types. In CHO/ETA cells, BQ-123, an ETA-selective antagonist, completely blocked ET-1-induced cPLA2 stimulation. In CHO/ETB cells, the ET-1 response was mimicked by 4AlaET-1 which could be blocked partially by PD 145065, a nonselective antagonist of ETA and ETB. As expected, ET-1 stimulated PGE2 synthesis in CHO cells transfected with ET receptors. We conclude that ET-1 can stimulate cPLA2 via both the human ETA and ETB receptor subtype.
内皮素-1（ET-1）激活胞质磷脂酶A2（cPLA2）的能力已在稳定表达人ETA（CHO/ETA）或人ETB（CHO/ETB）受体亚型的中国仓鼠卵巢（CHO）细胞中进行了研究。ET-1在两种细胞类型中均呈剂量依赖性增加二硫苏糖醇不敏感的cPLA2活性。在CHO/ETA细胞中，ETA选择性拮抗剂BQ-123完全阻断了ET-1诱导的cPLA2刺激。在CHO/ETB细胞中，4AlaET-1模拟了ET-1反应，该反应可被ETA和ETB的非选择性拮抗剂PD 145065部分阻断。正如预期的那样，ET-1刺激了转染了ET受体的CHO细胞中PGE2的合成。我们得出结论，ET-1可通过人ETA和ETB受体亚型刺激cPLA2。
