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索拉非尼（一种VEGFR-2和Raf激酶抑制剂）逆转转化生长因子-β诱导的肝细胞癌上皮-间质转化

Reversal of TGF-β-induced epithelial-mesenchymal transition in hepatocellular carcinoma by sorafenib, a VEGFR-2 and Raf kinase inhibitor.

作者信息

Modi Siddharth J, Tiwari Anshuly, Kulkarni Vithal M

机构信息

Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth (Deemed to be University), Pune, 411038, Maharashtra, India.

出版信息

Curr Res Pharmacol Drug Discov. 2021 Jan 19;2:100014. doi: 10.1016/j.crphar.2021.100014. eCollection 2021.

DOI:10.1016/j.crphar.2021.100014
PMID:34909649
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8663974/
Abstract

The epithelial-mesenchymal transition (EMT) is considered an essential process for cancer development and metastasis. Sorafenib, a RAF kinase and VEGFR-2 inhibitor, exhibits efficacy against advanced hepatocellular carcinoma (HCC), renal carcinoma, and thyroid cancer. It is well established that transforming growth factor-β (TGF-β) activated EMT is involved in the invasion and metastasis of Hep G2 cells in HCC. In this study, we investigated the effects of sorafenib on various biomarkers associated with EMT using flow cytometry. We found that sorafenib upregulated the epithelial marker E-cadherin and downregulated the mesenchymal marker vimentin. Furthermore, sorafenib downregulated the level of the EMT-inducing transcription factor SNAIL. Our findings provide insights into the mechanisms associated with the anti-EMT effects of VEGFR-2/RAF kinase inhibitors.

摘要

上皮-间质转化（EMT）被认为是癌症发展和转移的一个重要过程。索拉非尼是一种RAF激酶和VEGFR-2抑制剂，对晚期肝细胞癌（HCC）、肾癌和甲状腺癌具有疗效。众所周知，转化生长因子-β（TGF-β）激活的EMT参与了HCC中Hep G2细胞的侵袭和转移。在本研究中，我们使用流式细胞术研究了索拉非尼对与EMT相关的各种生物标志物的影响。我们发现索拉非尼上调上皮标志物E-钙黏蛋白并下调间质标志物波形蛋白。此外，索拉非尼下调了诱导EMT的转录因子SNAIL的水平。我们的研究结果为VEGFR-2/RAF激酶抑制剂的抗EMT作用相关机制提供了见解。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aab2/8663974/d1c4b3c7cc9b/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aab2/8663974/7a1069e7931e/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aab2/8663974/9b366729590b/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aab2/8663974/0fd21e602f80/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aab2/8663974/b325132c7c83/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aab2/8663974/7aaa7e7248e2/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aab2/8663974/d1c4b3c7cc9b/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aab2/8663974/7a1069e7931e/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aab2/8663974/9b366729590b/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aab2/8663974/0fd21e602f80/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aab2/8663974/b325132c7c83/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aab2/8663974/7aaa7e7248e2/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aab2/8663974/d1c4b3c7cc9b/gr5.jpg

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