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RGFP966通过在体外抑制肝癌细胞中表皮生长因子受体(EGFR)的表达来抑制肿瘤生长和迁移。

RGFP966 Suppresses Tumor Growth and Migration Through Inhibition of EGFR Expression in Hepatocellular Carcinoma Cells in vitro.

作者信息

Yu Xinying, Yang Fan, Jiang Hong, Fan Ling

机构信息

Second Pediatric Intensive Care Unit, Shengjing Hospital of China Medical University, Shenyang City, Liaoning Province, People's Republic of China.

Third Neonatal Ward, Shengjing Hospital of China Medical University, Shenyang City, Liaoning Province, People's Republic of China.

出版信息

Drug Des Devel Ther. 2020 Jan 10;14:121-128. doi: 10.2147/DDDT.S234871. eCollection 2020.

Abstract

PURPOSE

Histone deacetylase 3 (HDAC3) has been suggested to play a role in hepatocellular carcinoma (HCC). In the present report, we aimed to identify the effects of RGFP966, a specific HDAC3 inhibitor, on the cell proliferation and migration of HCC cell lines.

METHODS

Human HCC cell lines, which were identified using short tandem repeat (STR) DNA profiling analysis, were used in this report. Cell proliferation assay was used to identify the growth viability of cells. Wound healing and transwell assay were used to identify the migration ability of cells. Further, a human phospho-receptor tyrosine kinases array kit was used to screen out RGFP966 effects on key receptor tyrosine kinases. Then, the mRNA expression was quantified by real-time PCR, and protein expression was identified by Western blot immunoassay.

RESULTS

We found that RGFP966 inhibited both proliferation and migration of HCC cells. Further, RGFP966 represses the expression and phosphorylation levels of epidermal growth factor receptor (EGFR) in HCC cells. Moreover, HDAC3 is involved in the inhibition of EGFR by RGFP966. Overall, we elucidated an inhibitive function of RGFP966 in HCC progression.

CONCLUSION

RGFP966 inhibits EGFR signaling pathway and suppresses proliferation and migration of HCC cells.

摘要

目的

已有研究表明组蛋白去乙酰化酶3(HDAC3)在肝细胞癌(HCC)中发挥作用。在本报告中,我们旨在确定特异性HDAC3抑制剂RGFP966对肝癌细胞系细胞增殖和迁移的影响。

方法

本报告使用了通过短串联重复序列(STR)DNA谱分析鉴定的人肝癌细胞系。细胞增殖试验用于确定细胞的生长活力。伤口愈合试验和Transwell试验用于确定细胞的迁移能力。此外,使用人磷酸化受体酪氨酸激酶阵列试剂盒筛选RGFP966对关键受体酪氨酸激酶的影响。然后,通过实时PCR定量mRNA表达,并通过蛋白质印迹免疫测定法鉴定蛋白质表达。

结果

我们发现RGFP966抑制肝癌细胞的增殖和迁移。此外,RGFP966抑制肝癌细胞中表皮生长因子受体(EGFR)的表达和磷酸化水平。此外,HDAC3参与RGFP966对EGFR的抑制作用。总体而言,我们阐明了RGFP966在肝癌进展中的抑制功能。

结论

RGFP966抑制EGFR信号通路,抑制肝癌细胞的增殖和迁移。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b8d5/6959505/af59d57e7392/DDDT-14-121-g0001.jpg

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