Molecular identification and analysis of a novel human corticotropin-releasing factor (CRF) receptor: The CRF2γ receptor
Molecular identification and analysis of a novel human corticotropin-releasing factor (CRF) receptor: The CRF2γ receptor
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DOI：
10.1210/me.12.8.1077
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发表时间：
1998-08-01
影响因子：
--
通讯作者：
Largent, BL
中科院分区：
文献类型：
--
作者：
Kostich, WA;Chen, AR;Largent, BL
我们报告在人脑中发现了一种新的 CRF2 受体剪接亚型，我们将其称为 CRF2 γ 受体。 CRF2 γ cDNA 编码 397 个氨基酸的受体，其氨基末端与已报道的 α 和 β 末端没有显着同源性。当在 293-EBNA（Epstein-Barr 核抗原）细胞中表达时，CRF 受体以剂量依赖性方式对 CRF 和相关肽做出反应，尿皮质素的效力顺序大于或等于 sauvine>urotensin>r/h CRF，EC50 值与 CRF2 α 比 CRF2 β 更相似。使用放射性标记索瓦金的平衡饱和等温线分析揭示了与 CRF2 γ 结合的两个位点/状态模型，具有 60 pM K-d 高亲和力位点和 5 nM K-d 低亲和力位点。对人脑中 CRF2 γ RNA 表达的分析表明，在隔膜和海马中表达，在杏仁核、伏核、中脑和额叶皮质中表达较弱但可检测到。
We report the discovery of a new CRF2 receptor splice isoform found in human brain, which we have termed the CRF2 gamma receptor. The CRF2 gamma cDNA encodes for a 397-amino acid receptor that has an amino terminus with no significant homology to the already reported alpha- and beta-termini. When expressed in 293-EBNA (Epstein-Barr nuclear antigen) cells, the CRF,, receptor responds in a dose-dependent manner to CRF and related peptides with a rank order of potency of urocortin greater than or equal to sauvagine>urotensin>r/h CRF, with EC50 values more similar to CRF2 alpha than CRF2 beta. Equilibrium saturation isotherm analysis with radiolabeled sauvagine reveals a two site/state model for binding to CRF2 gamma with a 60 pM K-d high-affinity site and a 5 nM K-d low-affinity site. Analysis of CRF2 gamma RNA expression in human brain demonstrates expression in septum and hippocampus, with weaker but detectable expression in amygdala, nucleus accumbens, midbrain, and frontal cortex.