研究动态
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山奈酚对 TRPC5 的药理学操作可通过抑制参与丝状伪足形成的钙来减弱胃肠癌的转移。

Pharmacological manipulation of TRPC5 by kaempferol attenuates metastasis of gastrointestinal cancer via inhibiting calcium involved in the formation of filopodia.

发表日期:2024
作者: Suyun Yu, Rui Deng, Wei Wang, Defang Zou, Liang He, Zhonghong Wei, Yanhong Pan, Xiaoman Li, Yuanyuan Wu, Aiyun Wang, Wenxing Chen, Yang Zhao, Yin Lu
来源: International Journal of Biological Sciences

摘要:

热感觉受体、瞬时受体电位通道 5 (TRPC5) 是一种非选择性钙离子 (Ca2+) 渗透性离子通道,与癌症的发生和进展有关。然而,其在胃肠道癌症中的具体作用仍不清楚。这项研究表明,TRPC5 在胃肠道肿瘤中显着过度表达,并且与患者预后呈负相关。 TRPC5 过表达会引发细胞内 Ca2+ 水平 ([Ca2+]i) 大幅升高,驱动肌动蛋白细胞骨架重组并促进丝状伪足形成。此外,山奈酚是一种源自中药的化合物,被认为是一种TRPC5抑制剂,可以有效抑制其活性,从而阻止胃肠道癌症的转移。这些发现强调了 TRPC5 作为抑制转移的治疗靶点的潜力,而山奈酚正在成为一种有前途的天然抑制剂,可以优化用于预防癌症转移的临床应用。© 作者。
The thermo-sensory receptor, transient receptor potential channel 5 (TRPC5), a non-selective calcium ion (Ca2+)-permeable ion channel, has been implicated in cancer initiation and progression. However, its specific role in gastrointestinal cancer remains unclear. This study demonstrates that TRPC5 is significantly overexpressed in gastrointestinal tumors and is inversely associated with patient prognosis. TRPC5 overexpression triggers a substantial elevation in intracellular Ca2+ levels ([Ca2+]i), driving actin cytoskeleton reorganization and facilitating filopodia formation. Furthermore, kaempferol, a compound sourced from traditional Chinese medicine, is identified as a TRPC5 inhibitor that effectively suppresses its activity, thereby impeding gastrointestinal cancer metastasis. These findings underscore the potential of TRPC5 as a therapeutic target for metastasis inhibition, with kaempferol emerging as a promising natural inhibitor that could be optimized for clinical use in preventing cancer metastasis.© The author(s).