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首页> 外文期刊>Cellular Signalling >Functional characterization of neuropeptide 26RFa receptors GPR103A and GPR103B in zebrafish, Danio rerio
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Functional characterization of neuropeptide 26RFa receptors GPR103A and GPR103B in zebrafish, Danio rerio

机译：神经肽26RFA受体GPR103A和GPR103B在斑马鱼，Danio Rerio的功能表征

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摘要

The hypothalamic neuropeptide 26RFa is the most recently identified member of the RFamide peptide family, and this 26RFa signaling system has been shown to be implicated in regulating a variety of physiological processes. In zebrafish, 26RFa and two putative receptors, DrGPR103A and DrGPR103B, have been in silico identified, and in vivo data derived from overexpression and loss of function mutation experiments suggest the 26RFa signaling system plays an important role in the hypothalamic regulation of sleep. However, the biochemical and pharmacological information on DrGPR103A/B receptors is still unknown. Here, after cloning of cDNAs of two putative 26RFa receptor genes, DrGPR103A and B, from the total RNA of zebrafish whole body, functional assays demonstrated that both receptors were activated by synthetic zebrafish 26RFa neuropeptide, leading to a significant increase in CRE-driven luciferase activity and intracellular Ca2+ mobilization in a G(alpha q) inhibitor- and G(alpha i/o) inhibitor-sensitive manner. Upon activation by 26RFa, DrGPR103A and B evoked ERK1/2 phosphorylation and underwent internalization. Further functional determination also revealed that zebrafish kisspeptin-1 exhibited a slight potency for activating both DrGPR103A and B, and vice versa, zebrafish 26RFa also showed some activity at zebrafish GPR54A and B. Our findings provided evidence that zebrafish GPR103A and B are two functional G(alpha q)- and G(alpha i/o)-dually coupled receptors for 26RFa, enabling the further elucidation of the endocrinological roles of zebrafish 26RFa signaling system in the regulation of physiological activities.
机译：下丘脑神经肽26RFA是最近鉴定的rFamide肽家族的成员，并且该26RFA信号传导系统已被证明涉及调节各种生理过程。在斑马鱼中，26RFA和两个推定的受体，DRGPR103A和DRGPR103B已经鉴定在硅中，并且在源自过表达和功能突变实验的体内数据中，26RFA信号系统在睡眠中下丘脑调节中起重要作用。然而，DRGPR103A / B受体的生物化学和药理学信息仍然未知。这里，在克隆两种推定的26RFA受体基因的CDNA，DRGPR103a和B的CDNA，从斑马鱼全身的总RNA，功能测定证明，通过合成斑马鱼26RFA神经肽激活了两个受体，导致CRE驱动的荧光素酶显着增加在G（αQ）抑制剂和G（αI/ O）抑制剂敏感方式中的活性和细胞内Ca2 +动员。在66RFA的激活后，DRGPR103A和B诱发ERK1 / 2磷酸化并进行内化。进一步的功能确定还揭示了斑马鱼吻表表明，激活DRGPR103A和B的略微效力，反之亦然，斑马鱼26RFA也在斑马鱼GPR54A和B处展示了一些活性。我们的调查结果提供了斑马鱼GPR103A和B是两个功能G. （αQ） - 和G（αI/ o） - 26RFA的偶联受体，使斑马鱼26RFA信号传导系统的进一步阐明在生理活性调节中。

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  • 来源
    《Cellular Signalling》 |2020年第1期|共11页
  • 作者

    Wang Weiwei; Jiang Chaohui; Xu Yue; Ma Qiang; Yang Jingwen; Shi Ying; Zhou Naiming;

  • 作者单位

    Zhejiang Univ Coll Life Sci Inst Biochem Zijingang Campus Hangzhou 310058 Zhejiang Peoples R China;

    Zhejiang Univ Coll Life Sci Inst Biochem Zijingang Campus Hangzhou 310058 Zhejiang Peoples R China;

    Zhejiang Univ Coll Life Sci Inst Biochem Zijingang Campus Hangzhou 310058 Zhejiang Peoples R China;

    Zhejiang Univ Coll Life Sci Inst Biochem Zijingang Campus Hangzhou 310058 Zhejiang Peoples R China;

    Zhejiang Ocean Univ Marine Sci Coll Natl Engn Res Ctr Marine Facil Aquaculture Zhoushan 316022 Zhejiang Peoples R China;

    Zhejiang Univ Coll Life Sci Inst Biochem Zijingang Campus Hangzhou 310058 Zhejiang Peoples R China;

    Zhejiang Univ Coll Life Sci Inst Biochem Zijingang Campus Hangzhou 310058 Zhejiang Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 细胞形态学;
  • 关键词

    26RFa; Zebrafish; G-protein-coupled receptor (GPCR); Signal transduction; Neuropeptide;

    机译：26RFA;斑马鱼;G蛋白偶联受体（GPCR）;信号转导;神经肽;

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