Inhibition of SREBP-1 Activation by a Novel Small-Molecule Inhibitor Enhances the Sensitivity of Hepatocellular Carcinoma Tissue to Radiofrequency Ablation

Radiofrequency ablation (RFA) is an important strategy for treatment of advanced hepatocellular carcinoma (HCC). However, the prognostic indicators of RFA therapy are not known, and there are few strategies for RFA sensitization. The transcription factor sterol regulatory element binding protein 1 (...

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Autores principales: Xiao-zheng Zou, Jun-feng Hao, Xiu-hua Zhou
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Publicado: Frontiers Media S.A. 2021
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Acceso en línea:https://doaj.org/article/c3b72a56c4af459e972967d3937455c4
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spelling oai:doaj.org-article:c3b72a56c4af459e972967d3937455c42021-12-01T04:41:06ZInhibition of SREBP-1 Activation by a Novel Small-Molecule Inhibitor Enhances the Sensitivity of Hepatocellular Carcinoma Tissue to Radiofrequency Ablation2234-943X10.3389/fonc.2021.796152https://doaj.org/article/c3b72a56c4af459e972967d3937455c42021-11-01T00:00:00Zhttps://www.frontiersin.org/articles/10.3389/fonc.2021.796152/fullhttps://doaj.org/toc/2234-943XRadiofrequency ablation (RFA) is an important strategy for treatment of advanced hepatocellular carcinoma (HCC). However, the prognostic indicators of RFA therapy are not known, and there are few strategies for RFA sensitization. The transcription factor sterol regulatory element binding protein 1 (SREBP)-1 regulates fatty-acid synthesis but also promotes the proliferation or metastasis of HCC cells. Here, the clinical importance of SREBP-1 and potential application of knockdown of SREBP-1 expression in RFA of advanced HCC was elucidated. In patients with advanced HCC receiving RFA, a high level of endogenous SREBP-1 expression correlated to poor survival. Inhibition of SREBP-1 activation using a novel small-molecule inhibitor, SI-1, not only inhibited the aerobic glycolysis of HCC cells, it also enhanced the antitumor effects of RFA on xenograft tumors. Overall, our results: (i) revealed the correlation between SREBP-1 and HCC severity; (ii) indicated that inhibition of SREBP-1 activation could be a promising approach for treatment of advanced HCC.Xiao-zheng ZouJun-feng HaoXiu-hua ZhouFrontiers Media S.A.articlehepatocellular carcinomasterol regulatory element binding protein-1radiofrequency ablationaerobic glycolysissmall-molecule inhibitorRFA sensitizationNeoplasms. Tumors. Oncology. Including cancer and carcinogensRC254-282ENFrontiers in Oncology, Vol 11 (2021)
institution DOAJ
collection DOAJ
language EN
topic hepatocellular carcinoma
sterol regulatory element binding protein-1
radiofrequency ablation
aerobic glycolysis
small-molecule inhibitor
RFA sensitization
Neoplasms. Tumors. Oncology. Including cancer and carcinogens
RC254-282
spellingShingle hepatocellular carcinoma
sterol regulatory element binding protein-1
radiofrequency ablation
aerobic glycolysis
small-molecule inhibitor
RFA sensitization
Neoplasms. Tumors. Oncology. Including cancer and carcinogens
RC254-282
Xiao-zheng Zou
Jun-feng Hao
Xiu-hua Zhou
Inhibition of SREBP-1 Activation by a Novel Small-Molecule Inhibitor Enhances the Sensitivity of Hepatocellular Carcinoma Tissue to Radiofrequency Ablation
description Radiofrequency ablation (RFA) is an important strategy for treatment of advanced hepatocellular carcinoma (HCC). However, the prognostic indicators of RFA therapy are not known, and there are few strategies for RFA sensitization. The transcription factor sterol regulatory element binding protein 1 (SREBP)-1 regulates fatty-acid synthesis but also promotes the proliferation or metastasis of HCC cells. Here, the clinical importance of SREBP-1 and potential application of knockdown of SREBP-1 expression in RFA of advanced HCC was elucidated. In patients with advanced HCC receiving RFA, a high level of endogenous SREBP-1 expression correlated to poor survival. Inhibition of SREBP-1 activation using a novel small-molecule inhibitor, SI-1, not only inhibited the aerobic glycolysis of HCC cells, it also enhanced the antitumor effects of RFA on xenograft tumors. Overall, our results: (i) revealed the correlation between SREBP-1 and HCC severity; (ii) indicated that inhibition of SREBP-1 activation could be a promising approach for treatment of advanced HCC.
format article
author Xiao-zheng Zou
Jun-feng Hao
Xiu-hua Zhou
author_facet Xiao-zheng Zou
Jun-feng Hao
Xiu-hua Zhou
author_sort Xiao-zheng Zou
title Inhibition of SREBP-1 Activation by a Novel Small-Molecule Inhibitor Enhances the Sensitivity of Hepatocellular Carcinoma Tissue to Radiofrequency Ablation
title_short Inhibition of SREBP-1 Activation by a Novel Small-Molecule Inhibitor Enhances the Sensitivity of Hepatocellular Carcinoma Tissue to Radiofrequency Ablation
title_full Inhibition of SREBP-1 Activation by a Novel Small-Molecule Inhibitor Enhances the Sensitivity of Hepatocellular Carcinoma Tissue to Radiofrequency Ablation
title_fullStr Inhibition of SREBP-1 Activation by a Novel Small-Molecule Inhibitor Enhances the Sensitivity of Hepatocellular Carcinoma Tissue to Radiofrequency Ablation
title_full_unstemmed Inhibition of SREBP-1 Activation by a Novel Small-Molecule Inhibitor Enhances the Sensitivity of Hepatocellular Carcinoma Tissue to Radiofrequency Ablation
title_sort inhibition of srebp-1 activation by a novel small-molecule inhibitor enhances the sensitivity of hepatocellular carcinoma tissue to radiofrequency ablation
publisher Frontiers Media S.A.
publishDate 2021
url https://doaj.org/article/c3b72a56c4af459e972967d3937455c4
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AT junfenghao inhibitionofsrebp1activationbyanovelsmallmoleculeinhibitorenhancesthesensitivityofhepatocellularcarcinomatissuetoradiofrequencyablation
AT xiuhuazhou inhibitionofsrebp1activationbyanovelsmallmoleculeinhibitorenhancesthesensitivityofhepatocellularcarcinomatissuetoradiofrequencyablation
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