Prostaglandin E receptor EP3 gamma isoform, with mostly full constitutive Gi activity and agonist-dependent Gs activity

Prostaglandin E receptor EP3 gamma isoform, with mostly full constitutive Gi activity and agonist-dependent Gs activity
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DOI:
10.1016/0014-5793(96)00354-7
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发表时间:
1996-05-20
期刊:
影响因子:
3.5
通讯作者:
Ichikawa, A
Ichikawa, A
中科院分区:
生物学3区
文献类型:
--
作者:
Negishi, M;Hasegawa, H;Ichikawa, A

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我们最近证明,具有不同羧基末端尾的小鼠EP 3受体的两种专门的Gi偶联同种型EP 3 α和β在激动剂非依赖性组成型Gi活性方面不同,并且羧基末端尾截短的受体显示完全的组成型活性(Hasegawa,H.,Negishi,M.,和Ichikawa,A.(1996)J.Biol.Chem.271,1857-1860)。在此,我们进一步检查了与Gi和Gs两者偶联的第三种亚型EP 3 γ的Gi和Gs活性。EP 3 γ受体显示了大部分完全的组成型Gi活性和激动剂依赖性Gs活性。截短的受体也显示了激动剂依赖性Gs活性,但水平低于EP 3 γ受体的活性。羧基末端尾将差异调节EP 3受体的Gi和Gs活性。
We recently demonstrated that two exclusively Gi-coupled isoforms of the mouse EP3 receptor, EP3 alpha and beta, with different carboxyl-terminal tails, differed in agonist-independent constitutive Gi activity, and the carboxyl-terminal tail-truncated receptor showed full constitutive activity (Hasegawa, H., Negishi, M., and Ichikawa, A. (1996) J. Biol. Chem. 271, 1857-1860). Here we further examined Gi and Gs activities of the third isoform, EP3 gamma, coupled to both Gi and Gs, The EP3 gamma receptor showed mostly full constitutive Gi activity and agonist-dependent Gs activity, The truncated receptor also showed agonist-dependent Gs activity, but the level was lower than that of the EP3 gamma receptor, Thus, the carboxyl-terminal tail would differentially regulate Gi and Gs activities of the EP3 receptor.