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Journal of Experimental & Clinical Cancer Research

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Open Access 01-12-2021 | Research

Cirsiliol targets tyrosine kinase 2 to inhibit esophageal squamous cell carcinoma growth in vitro and in vivo

Authors: Xuechao Jia, Chuntian Huang, Yamei Hu, Qiong Wu, Fangfang Liu, Wenna Nie, Hanyong Chen, Xiang Li, Zigang Dong, Kangdong Liu

Published in: Journal of Experimental & Clinical Cancer Research | Issue 1/2021

Abstract

Background

Esophageal squamous cell carcinoma (ESCC) is an aggressive and lethal cancer with a low 5 year survival rate. Identification of new therapeutic targets and its inhibitors remain essential for ESCC prevention and treatment.

Methods

TYK2 protein levels were checked by immunohistochemistry. The function of TYK2 in cell proliferation was investigated by MTT [(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] and anchorage-independent cell growth. Computer docking, pull-down assay, surface plasmon resonance, and kinase assay were used to confirm the binding and inhibition of TYK2 by cirsiliol. Cell proliferation, western blot and patient-derived xenograft tumor model were used to determine the inhibitory effects and mechanism of cirsiliol in ESCC.

Results

TYK2 was overexpressed and served as an oncogene in ESCC. Cirsiliol could bind with TYK2 and inhibit its activity, thereby decreasing dimer formation and nucleus localization of signal transducer and activator of transcription 3 (STAT3). Cirsiliol could inhibit ESCC growth in vitro and in vivo.

Conclusions

TYK2 is a potential target in ESCC, and cirsiliol could inhibit ESCC by suppression of TYK2.

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Title: Cirsiliol targets tyrosine kinase 2 to inhibit esophageal squamous cell carcinoma growth in vitro and in vivo
Authors: Xuechao Jia
Chuntian Huang
Yamei Hu
Qiong Wu
Fangfang Liu
Wenna Nie
Hanyong Chen
Xiang Li
Zigang Dong
Kangdong Liu
Publication date: 01-12-2021
Publisher: BioMed Central
Published in: Journal of Experimental & Clinical Cancer Research / Issue 1/2021
Electronic ISSN: 1756-9966
DOI: https://doi.org/10.1186/s13046-021-01903-z

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Abstract

Background

Methods

Results

Conclusions

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