前列腺素E受体EP3亚型同工型以不同效率增强腺苷酸环化酶刺激作用。
Enhancement of adenylate cyclase stimulation by prostaglandin E receptor EP3 subtype isoforms with different efficiencies.
作者信息
Harazono A, Sugimoto Y, Ichikawa A, Negishi M
机构信息
Department of Physiological Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University, Japan.
出版信息
Biochem Biophys Res Commun. 1994 May 30;201(1):340-5. doi: 10.1006/bbrc.1994.1707.
We recently cloned the mouse prostaglandin (PG) E receptor EP3 subtype that is coupled to adenylate cyclase inhibition through Gi and identified two isoforms of EP3, EP3 alpha and EP3 beta, which are produced through alternative splicing and differ only in the carboxyl-terminal domain. Preincubation of Chinese hamster ovary cells expressing each isoform with PGE2 concentration-dependently enhanced both the basal and forskolin-stimulated cAMP formation, but two orders higher concentrations of PGE2 were required for EP3 beta than EP3 alpha for 50% enhancement of both formations. This enhancement by EP3 isoforms was completely blocked by pertussis toxin treatment, indicating that it is mediated through Gi activation. Thus, the two EP3 isoforms with different carboxyl-terminal tails induce enhancement of adenylate cyclase stimulation with different efficiencies.
我们最近克隆了小鼠前列腺素（PG）E受体EP3亚型，该亚型通过Gi与腺苷酸环化酶抑制偶联，并鉴定出EP3的两种亚型，即EP3α和EP3β，它们通过可变剪接产生，仅在羧基末端结构域有所不同。用PGE2对表达每种亚型的中国仓鼠卵巢细胞进行预孵育，可浓度依赖性地增强基础和福斯可林刺激的cAMP生成，但对于两种生成的50%增强，EP3β所需的PGE2浓度比EP3α高两个数量级。EP3亚型的这种增强作用在百日咳毒素处理后完全被阻断，表明它是通过Gi激活介导的。因此，具有不同羧基末端尾巴的两种EP3亚型以不同效率诱导腺苷酸环化酶刺激增强。
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