1. bookVolume 72 (2022): Issue 3 (September 2022)
Journal Details
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Format
Journal
eISSN
1846-9558
First Published
28 Feb 2007
Publication timeframe
4 times per year
Languages
English
access type Open Access

Fingolimod exerts in vitro anticancer activity against hepatocellular carcinoma cell lines via YAP/TAZ suppression

Published Online: 13 Apr 2022
Volume & Issue: Volume 72 (2022) - Issue 3 (September 2022)
Page range: 427 - 436
Accepted: 19 Jan 2022
Journal Details
License
Format
Journal
eISSN
1846-9558
First Published
28 Feb 2007
Publication timeframe
4 times per year
Languages
English
Abstract

Hepatocellular carcinoma (HCC) remains a notably global health challenge with high mortality rates and poor prognosis. The deregulation of the Hippo signalling pathway, especially the overexpression and activation of downstream effector Yes-associated protein (YAP), has been demonstrated to result in the rapid malignant evolution of HCC. In this context, multiple efforts have been dedicated to targeting YAP for HCC therapy, but effective YAP inhibitors are still lacking. In this study, through a YAP-TEAD (8×GTIIC) luciferase reporter assay, we identified fingolimod, an immunomodulatory drug approved for the treatment of multiple sclerosis, as a novel YAP inhibitor. Fingolimod suppressed the proliferation of HCC cell lines by downregulating the protein levels as well as the trans-activating function of YAP. Overall, our current study not only identifies fingolimod as a novel YAP-targeting in hibitor, but also indicates that this clinically-approved drug could be utilized as a potential and feasible therapeutic drug for HCC.

Keywords

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