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首页> 外文期刊>Cellular Signalling >Homologous and heterologous phosphorylation of the vasopressin V1a receptor.
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Homologous and heterologous phosphorylation of the vasopressin V1a receptor.

机译：加压素V1a受体的同源和异源磷酸化。

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摘要

The vasopressin V1a receptor undergoes homologous and heterologous desensitizations which can be mimicked by activation of protein kinase C. This suggests that phosphorylation of the V1a receptor may be involved in the desensitization mechanisms. Such a phosphorylation was presently investigated in HEK 293 cells stably transfected with rat vasopressin V1a receptor. Metabolic labelling and immunoprecipitation of epitope-tagged V1a receptor evidenced a 52-kDa band and a 92-kDa band. Glycosidase treatments and immunoblotting experiments suggest that the 52-kDa band corresponds to an immature unprocessed receptor protein, whereas the 92-kDa band would correspond to a highly glycosylated form of the mature V1a receptor. Exposure of the cells to vasopressin induced a selective 32P phosphate incorporation in the 92-kDa form of the receptor. This homologous ligand-induced phosphorylation was dose dependent with maximal phosphate incorporation corresponding to four times the basal level. Stimulation of the endogenous phospholipase C-coupled m3 muscarinic receptor by carbachol-induced heterologous phosphorylation of the V1a receptor whose amplitude was half that of the homologous phosphorylation. This heterologous phosphorylation was associated with a reduced vasopressin-dependent increase in intracellular calcium.
机译：血管加压素V1a受体经历了同源和异源脱敏作用，可以通过激活蛋白激酶C来模拟。这表明V1a受体的磷酸化可能参与了脱敏作用机理。目前在用大鼠血管加压素V1a受体稳定转染的HEK 293细胞中研究了这种磷酸化。带有表位标记的V1a受体的代谢标记和免疫沉淀显示出一条52 kDa的条带和一条92 kDa的条带。糖苷酶处理和免疫印迹实验表明，52 kDa的条带对应于未成熟的未加工受体蛋白，而92 kDa的条带对应于成熟的V1a受体的高度糖基化形式。将细胞暴露于加压素会诱导受体92-kDa形式的选择性32P磷酸盐结合。这种同源的配体诱导的磷酸化是剂量依赖性的，最大磷酸盐掺入量是基础水平的四倍。卡巴胆碱引起的V1a受体异源磷酸化刺激内源磷脂酶C偶联的m3毒蕈碱受体，其幅度是同源磷酸化幅度的一半。这种异源磷酸化与减少的细胞内钙加压素依赖性增加有关。

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