摘要
瞬时感受器电位melastatin 7(TRPM7)是一种能与功能激酶结构域融合的非选择性阳离子通道。在生理上,TRPM7通道参与镁代谢、细胞存活和原肠胚形成。细胞内镁及镁复合核苷酸通过TRPM7通道抑制离子电流。同时,该激酶能够磷酸化的细胞骨架蛋白如肌球蛋白链调节细胞的张力和蠕动。此外,TRPM7激酶可被caspase裂解,参与细胞凋亡的信号传导。要的是,TRPM7通道表达在许多肿瘤中,如乳腺癌、胶质母细胞瘤、鼻咽癌、卵巢异常,胰腺癌等。此外,TRPM7的高表达是乳腺癌预后的一个独立的生物标志物。药理调制或TRPM7的抑制影响肿瘤细胞的增殖、粘附、迁移和侵袭能力。尽管如此, TRPM7通道干扰癌细胞的机制仍不明确。在本综述中,我们将探讨TRPM7通道在肿瘤中的作用。特别是,我们将区分离子信号和激酶的功能,以便更好地了解TRPM7通道在癌症的发展中发挥的核心作用。我们还将讨论RPM7的药物阻断剂和其对癌症治疗的潜在作用剂的研究进展。
关键词: TRPM7、上皮癌、钙、镁、激酶、药理拮抗剂。
Current Medicinal Chemistry
Title:Recent Advances in Oncogenic Roles of the TRPM7 Chanzyme
Volume: 23 Issue: 36
Author(s): Mathieu Gautier, Marianne Perrière, Michael Monet, Alison Vanlaeys, Irina Korichneva, Isabelle Dhennin-Duthille and Halima Ouadid-Ahidouch
Affiliation:
关键词: TRPM7、上皮癌、钙、镁、激酶、药理拮抗剂。
摘要: Transient Receptor Potential Melastatin-related 7 (TRPM7) is a non-selective cation channel fused with a functional kinase domain. Physiologically, TRPM7 channel is involved in magnesium homeostasis, cell survival and gastrulation. The channel part is responsible for calcium, magnesium, and metal trace entries. Cation current through TRPM7 channel is inhibited by both intracellular magnesium and magnesium complexed with nucleotides. In parallel, the kinase is able to phosphorylate cytoskeleton proteins like myosin chain regulating cell tension and motility. Moreover, TRPM7 kinase domain can be cleaved by caspase and participates to apoptosis signaling. Importantly, TRPM7 channel expression is aberrant in numerous cancers including breast, glioblastoma, nasopharynx, ovarian, and pancreatic. Moreover, TRPM7 high expression is an independent biomarker of poor outcome in breast cancer. Pharmacological modulation or silencing of TRPM7 strongly affects proliferation, adhesion, migration or invasion in cancer cell lines. Nevertheless, it is still not clear by which mechanism TRPM7 channels may disturb cancer cell hallmarks. In the present review, we will discuss the role of TRPM7 channels in malignancies. In particular, we will distinguish the role of cation signaling from kinase function in order to better understand how TRPM7 channels may play a central role in cancer progression. We will also discuss the recent advances in pharmacological blockers of TRPM7 and their potential use for cancer therapy.
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Mathieu Gautier, Marianne Perrière, Michael Monet, Alison Vanlaeys, Irina Korichneva, Isabelle Dhennin-Duthille and Halima Ouadid-Ahidouch , Recent Advances in Oncogenic Roles of the TRPM7 Chanzyme, Current Medicinal Chemistry 2016; 23 (36) . https://dx.doi.org/10.2174/0929867323666160907162002
DOI https://dx.doi.org/10.2174/0929867323666160907162002 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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