Natural and Synthetic Modulators of the TRPM7 Channel.
Natural and Synthetic Modulators of the TRPM7 Channel.
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DOI：
10.3390/cells3041089
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发表时间：
2014-11-27
期刊：
影响因子：
6
通讯作者：
Gudermann T
中科院分区：
文献类型：
--
作者：
Chubanov V;Schäfer S;Ferioli S;Gudermann T
瞬时受体电位阳离子通道亚家族 M 成员 7 (TRPM7) 是一种双功能蛋白，包含与 α 型蛋白激酶结构域连接的 TRP 离子通道片段。 TRPM7 的基因失活揭示了其在镁代谢、细胞运动、增殖和分化中的核心作用。 TRPM7 与缺氧神经元死亡、心脏纤维化和肿瘤进展相关，凸显 TRPM7 作为新的药物靶点。最近，多个实验室独立鉴定出抑制或激活 TRPM7 通道的药理学化合物。最近发现的 TRPM7 调节剂被用作新的实验工具来阐明 TRPM7 通道的细胞功能。在这里，我们对这个新兴领域进行了简要概述。
Transient receptor potential cation channel subfamily M member 7 (TRPM7) is a bi-functional protein comprising a TRP ion channel segment linked to an α-type protein kinase domain. Genetic inactivation of TRPM7 revealed its central role in magnesium metabolism, cell motility, proliferation and differentiation. TRPM7 is associated with anoxic neuronal death, cardiac fibrosis and tumor progression highlighting TRPM7 as a new drug target. Recently, several laboratories have independently identified pharmacological compounds inhibiting or activating the TRPM7 channel. The recently found TRPM7 modulators were used as new experimental tools to unravel cellular functions of the TRPM7 channel. Here, we provide a concise overview of this emerging field.