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RGS6 通过促进 Tip60 介导的 Dnmt1 降解和促进细胞凋亡来抑制 Ras 诱导的细胞转化。

RGS6 suppresses Ras-induced cellular transformation by facilitating Tip60-mediated Dnmt1 degradation and promoting apoptosis.

机构信息

Department of Pharmacology, Roy J. and Lucille A. Carver College of Medicine, University of Iowa, Iowa City, IA, USA.

Department of Biochemistry, Roy J. and Lucille A. Carver College of Medicine, University of Iowa, Iowa City, IA, USA.

出版信息

Oncogene. 2014 Jul 3;33(27):3604-11. doi: 10.1038/onc.2013.324. Epub 2013 Sep 2.

Abstract

The RAS protooncogene has a central role in regulation of cell proliferation, and point mutations leading to oncogenic activation of Ras occur in a large number of human cancers. Silencing of tumor-suppressor genes by DNA methyltransferase 1 (Dnmt1) is essential for oncogenic cellular transformation by Ras, and Dnmt1 is overexpressed in numerous human cancers. Here we provide new evidence that the pleiotropic regulator of G protein signaling (RGS) family member RGS6 suppresses Ras-induced cellular transformation by facilitating Tip60-mediated degradation of Dmnt1 and promoting apoptosis. Employing mouse embryonic fibroblasts from wild-type and RGS6(-/-) mice, we found that oncogenic Ras induced upregulation of RGS6, which in turn blocked Ras-induced cellular transformation. RGS6 functions to suppress cellular transformation in response to oncogenic Ras by downregulating Dnmt1 protein expression leading to inhibition of Dnmt1-mediated anti-apoptotic activity. Further experiments showed that RGS6 functions as a scaffolding protein for both Dnmt1 and Tip60 and is required for Tip60-mediated acetylation of Dnmt1 and subsequent Dnmt1 ubiquitylation and degradation. The RGS domain of RGS6, known only for its GTPase-activating protein activity toward Gα subunits, was sufficient to mediate Tip60 association with RGS6. This work demonstrates a novel signaling action for RGS6 in negative regulation of oncogene-induced transformation and provides new insights into our understanding of the mechanisms underlying Ras-induced oncogenic transformation and regulation of Dnmt1 expression. Importantly, these findings identify RGS6 as an essential cellular defender against oncogenic stress and a potential therapeutic target for developing new cancer treatments.

摘要

RAS 原癌基因在细胞增殖的调节中起着核心作用,导致 Ras 致癌激活的点突变发生在大量人类癌症中。DNA 甲基转移酶 1(Dnmt1)通过 Ras 沉默肿瘤抑制基因对于致癌细胞转化是必不可少的,并且 Dnmt1 在许多人类癌症中过度表达。在这里,我们提供了新的证据表明,G 蛋白信号转导的多效调节剂(RGS)家族成员 RGS6 通过促进 Tip60 介导的 Dmnt1 降解和促进细胞凋亡来抑制 Ras 诱导的细胞转化。利用来自野生型和 RGS6(-/-)小鼠的胚胎成纤维细胞,我们发现致癌 Ras 诱导 RGS6 的上调,反过来又阻断 Ras 诱导的细胞转化。RGS6 通过下调 Dnmt1 蛋白表达来抑制 Dnmt1 介导的抗凋亡活性,从而响应致癌 Ras 抑制细胞转化。进一步的实验表明,RGS6 作为 Dnmt1 和 Tip60 的支架蛋白发挥作用,并且是 Tip60 介导的 Dnmt1 乙酰化和随后的 Dnmt1 泛素化和降解所必需的。RGS6 的 RGS 结构域仅因其对 Gα亚基的 GTPase 激活蛋白活性而被知晓,足以介导 Tip60 与 RGS6 的关联。这项工作证明了 RGS6 在负向调节致癌基因诱导的转化中的一种新的信号作用,并为我们理解 Ras 诱导的致癌转化和 Dnmt1 表达调控的机制提供了新的见解。重要的是,这些发现确定 RGS6 是一种对抗致癌应激的重要细胞防御机制,并为开发新的癌症治疗方法提供了一个潜在的治疗靶点。

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