The aryl hydrocarbon receptor ligand ITE inhibits cell proliferation and migration and enhances sensitivity to drug-resistance in hepatocellular carcinoma.

Journal of Cellular Physiology
Xiaoqian ZhangLanjuan Li

Abstract

Aryl hydrocarbon receptor (AHR), a ligand-activated transcription factor, is considered as a crucial gene during tumor formation and progress. Among various ligands, 2-(1'H-indole-3'-carbonyl)-thiazole-4-carboxylic acid methyl ester (ITE) has been evaluated to share a broad spectrum of biological activities. However, the specific effects and potential mechanisms of ITE against hepatocellular carcinoma remain unclear. Here we explored whether ITE exerted antitumor activity against hepatocellular carcinoma (HCC) cells and its potential mechanisms in vitro and in vivo. We found that ITE could markedly inhibit proliferation of HCCLM3 and SMMC-7721 cells and induce G0/G1 arrest and apoptosis with alterations of expressions of the related proteins. Also, ITE could prohibit the process of migration and invasion evaluated by transwell assay. Moreover, ITE exhibited remarkable capability to repress the growth of HCCLM3-SR cells and induce apoptosis in contrast to sorafenib. Additionally, ITE also showed potent antitumor activity against the HCCLM3 xenograft by prohibiting tumor growth without any toxicity to mice. Mechanistically, AHR activation by ITE was attributed to inhibition of HCC cells as AHR knockdown would abolish ITE-induced ...Continue Reading

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Citations

Jul 3, 2021·International Journal of Molecular Sciences·Yujie Yang, William K Chan

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