Induction of prostacyclin receptor expression in human erythroleukemia cells

FEBS Letters

Murray, Rosemary¹  FitzGerald, Garret A.¹  Furci, Lucinda¹ 

[1] Division of Clinical Pharmacology, Vanderbilt University, Nashville, TN 37232, USA

关键词: Prostacyclin receptor;    Phorbol ester;    Adenylate cyclase;   

DOI  :  10.1016/0014-5793(89)81084-1

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

We have identified both high-affinity (K_D = 36±3 nM) and low-affinity (K_D = 2.1±0.8 μM) 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-G_s-adenylate cyclase system. HEL cells represent a source of prostacyclin receptor mRNA which may be of value in expression cloning of this receptor.

【 授权许可】

Unknown