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瞬时受体电位 melastatin 7 及其调节剂。

Transient receptor potential melastatin 7 and their modulators.

机构信息

The Second School of Clinical Medicine, Anhui Medical University, Hefei, 230032, China.

Department of Clinical Pharmacology, The Second Hospital of Anhui Medical University, Hefei, 230601, China.

出版信息

Eur J Pharmacol. 2022 Sep 15;931:175180. doi: 10.1016/j.ejphar.2022.175180. Epub 2022 Aug 5.

Abstract

TRPM (transient receptor potential melastatin) 7, a member of the TRPM subfamily, is a nonselective cation channel located on the cell membrane that regulates mammalian cell intracellular Mg balance. TRPM7 is widely expressed in vivo and is characterized by a unique domain structure comprised of cation channel and protein kinase. TRPM7 primarily controls the cellular influx of Mg and Ca. As such TRPM7 plays an important role in the physiological processes of cell proliferation, adhesion, migration, and differentiation, as well as phenotypic transformation. Changes in TRPM7 expression and activity are directly related to diseases such as tissue fibrosis, vascular injury, as well as the occurrence and development of tumors. The structure and function of TRPM7 has been previously described, but regulation of TRPM7 has been limited to Mg and laboratory pharmacological compounds. Hence, in this review, we summarized the endogenous and exogenous regulation of TRPM7, clarified its internal regulatory mechanisms and molecular signaling pathways, and emphasized the regulation of TRPM7 activity as an important target for disease treatment.

摘要

瞬时受体电位 M 亚家族 7 型(TRPM7)是位于细胞膜上的非选择性阳离子通道,调节哺乳动物细胞内镁平衡。TRPM7 在体内广泛表达,其特征是由阳离子通道和蛋白激酶组成的独特结构域。TRPM7 主要控制细胞内镁和钙的内流。因此,TRPM7 在细胞增殖、黏附、迁移和分化以及表型转化等生理过程中发挥着重要作用。TRPM7 表达和活性的变化与组织纤维化、血管损伤以及肿瘤的发生和发展等疾病直接相关。TRPM7 的结构和功能以前已有描述,但对 TRPM7 的调节仅限于镁和实验室药理学化合物。因此,在这篇综述中,我们总结了 TRPM7 的内源性和外源性调节,阐明了其内部调节机制和分子信号通路,并强调了 TRPM7 活性的调节作为疾病治疗的重要靶点。

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