Modulation of forskolin-mediated adenylyl cyclase activation by constitutively active GS-coupled receptors
Modulation of forskolin-mediated adenylyl cyclase activation by constitutively active GS-coupled receptors
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DOI：
10.1016/s0014-5793(97)01440-3
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发表时间：
1997-12-15
期刊：
影响因子：
3.5
通讯作者：
Leurs, R
中科院分区：
文献类型：
--
作者：
Alewijnse, AE;Smit, MJ;Leurs, R
在转染组胺H-2受体的CHO细胞中，组胺H-2受体的活性不仅增加了基础cAMP水平，而且增加了Forsklin诱导的cAMP生成。相反的H-2激动剂抑制了增加的Forsklin反应，其效力与基础水平测定的结果相似。在HEK-293和Sf9细胞中表达H-2受体或在COS-7细胞中表达TSH受体后，也观察到Forsklin反应的调制。Forsklin诱导的cAMP产生的增加似乎是结构性活性G(S)偶联受体的一个共同特征，对研究野生型受体的反向兴奋非常有用。(C)1997年欧洲生化学会联合会。
In transfected CHO cells constitutively active histamine H-2 receptors not only increase the basal cAMP level, but also enhance forskolin-induced cAMP production. The increased forskolin response was inhibited by inverse H-2 agonists with potencies similar to those determined at basal levels. The modulation of the forskolin response was also observed after H-2 receptor expression in HEK-293 and Sf9 cells or TSH receptor expression in COS-7 cells, The enhancement of forskolin-induced cAMP production seems to be a general characteristic of constitutively active G(s)-coupled receptors and can be very useful to study inverse agonism at wild-type receptors. (C) 1997 Federation of European Biochemical Societies.