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先前假定的GPR4“不依赖配体”信号传导是通过质子感应机制介导的。

Previously postulated "ligand-independent" signaling of GPR4 is mediated through proton-sensing mechanisms.

作者信息

Tobo Masayuki, Tomura Hideaki, Mogi Chihiro, Wang Ju-Qiang, Liu Jin-Peng, Komachi Mayumi, Damirin Alatangaole, Kimura Takao, Murata Naoya, Kurose Hitoshi, Sato Koichi, Okajima Fumikazu

机构信息

Laboratory of Signal Transduction, Institute for Molecular and Cellular Regulation, Gunma University, 3-39-15 Showa-machi, Maebashi 371-8512, Japan.

出版信息

Cell Signal. 2007 Aug;19(8):1745-53. doi: 10.1016/j.cellsig.2007.03.009. Epub 2007 Mar 30.

Abstract

GPR4 was initially identified as a receptor for sphingosylphosphorylcholine and lysophosphatidylcholine; however, lipid actions have not always been confirmed. Instead, ligand-independent actions have sometimes been observed in GPR4- and other OGR1 family receptor-expressing cells. Here, we examined the possible involvement of extracellular protons, which have recently been proposed as another ligand for GPR4. At pH 7.4, the epidermal growth factor-induced extracellular signal-regulated kinase activity was lower in GPR4-transfected RH7777 cells, in association with increased cAMP accumulation, than in vector-transfected cells. The serum response element (SRE)-driven transcriptional activity was also clearly higher in GPR4-expressing HEK293 cells than in vector-transfected cells at pH 7.4. These apparent ligand-independent actions were very small at alkalinic 7.8. The SRE activity was further increased by extracellular acidification in a manner dependent on the G13 protein/Rho signaling pathway in HEK293 cells expressing GPR4 or other OGR1 receptor family members. GPR4-expressing cells also showed a calcineurin-dependent nuclear factor of activated T cell (NFAT) promoter activation at pH 7.4, and this activity was further increased by pH below 7.2 in association with inositol phosphate production. In contrast to the cAMP and SRE responses, however, alkalinization to pH 7.8 hardly affected the high basal activity. Finally, the expression of GPR4 hardly modulated the sphingosylphosphorylcholine- or lysophosphatidylcholine-induced action. These results suggest that an extracellular proton play a role as a ligand in some of previously postulated ligand-independent actions through GPR4 receptors. Moreover, GPR4 may be a multi-functional receptor coupling to Gs, G13, and Gq/11 proteins in response to extracellular acidification.

摘要

GPR4最初被鉴定为鞘氨醇磷酸胆碱和溶血磷脂酰胆碱的受体;然而,脂质作用并非总能得到证实。相反,在表达GPR4和其他OGR1家族受体的细胞中,有时会观察到非配体依赖性作用。在此,我们研究了细胞外质子作为GPR4另一配体的可能性,细胞外质子最近被提出可能是GPR4的配体。在pH 7.4时,与载体转染细胞相比,在转染GPR4的RH7777细胞中,表皮生长因子诱导的细胞外信号调节激酶活性较低,同时伴有cAMP积累增加。在pH 7.4时,血清反应元件(SRE)驱动的转录活性在表达GPR4的HEK293细胞中也明显高于载体转染细胞。在碱性pH 7.8时,这些明显的非配体依赖性作用非常小。在表达GPR4或其他OGR1受体家族成员的HEK293细胞中,细胞外酸化以依赖G13蛋白/Rho信号通路的方式进一步增加了SRE活性。表达GPR4的细胞在pH 7.4时也显示出钙调神经磷酸酶依赖性的活化T细胞核因子(NFAT)启动子激活,并且在pH低于7.2时,这种活性会随着肌醇磷酸的产生而进一步增加。然而,与cAMP和SRE反应不同,碱化至pH 7.8几乎不影响高基础活性。最后,GPR4的表达几乎不调节鞘氨醇磷酸胆碱或溶血磷脂酰胆碱诱导的作用。这些结果表明,细胞外质子在一些先前假定的通过GPR4受体的非配体依赖性作用中作为配体发挥作用。此外,GPR4可能是一种多功能受体,在细胞外酸化时与Gs、G13和Gq/11蛋白偶联。

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