人红白血病细胞中前列环素受体表达的诱导
Induction of prostacyclin receptor expression in human erythroleukemia cells.
作者信息
Murray R, Furci L, FitzGerald G A
机构信息
Division of Clinical Pharmacology, Vanderbilt University, Nashville, TN 37232.
出版信息
FEBS Lett. 1989 Sep 11;255(1):172-4. doi: 10.1016/0014-5793(89)81084-1.
We have identified both high-affinity (KD = 36 +/- 3 nM) and low-affinity (KD = 2.1 +/- 0.8 microM) prostacyclin (PGI2)-receptor sites on human erythroleukemia (HEL) cells using the radiolabelled prostacyclin analogue. [3H]iloprost. The addition of the phorbol ester, TPA, to the culture medium caused a 5-10-fold increase in the number of both the low- and the high-affinity sites, without any change in their affinity constants. Iloprost stimulated HEL cell membrane adenylate cyclase activity 5-fold. This stimulation was potentiated in the presence of GTP, indicating a conventional PGI2 receptor-G2-adenylate cyclase system. HEL cells represent a source of prostacyclin receptor mRNA which may be of value in expression cloning of this receptor.
我们使用放射性标记的前列环素类似物[3H]伊洛前列素，在人红白血病（HEL）细胞上鉴定出了高亲和力（KD = 36±3 nM）和低亲和力（KD = 2.1±0.8 μM）的前列环素（PGI2）受体位点。向培养基中添加佛波酯TPA会使低亲和力和高亲和力位点的数量增加5至10倍，而它们的亲和常数没有任何变化。伊洛前列素可使HEL细胞膜腺苷酸环化酶活性提高5倍。在GTP存在的情况下，这种刺激作用增强，表明存在传统的PGI2受体 - G蛋白 - 腺苷酸环化酶系统。HEL细胞是前列环素受体mRNA的一个来源，这在该受体的表达克隆中可能具有价值。
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