Binding and ubiquitination-mediated degradation of ACKR3 by the novel Scutellarein derivative TBS6b potently suppresses hepatocellular carcinoma

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成果类型：

期刊论文

作者：

Jiang, Xing;Liang, Ying;Tang, Guotao;Quan, Haiyan;Ruan, Lijun;...

通讯作者：

Wu, Fangfang;Yang, Xiaonan

作者机构：

[Song, Zhijun; Zhang, Mengli; Tan, Zhien; Lu, Na; Jiang, Xing; Ou, Min; Wu, Fangfang; Ruan, Lijun; Liang, Ying] National Engineering Research Center for Southwest Endangered Medicinal Resources Development, Guangxi Key Laboratory of Medicinal Resources Protection and Genetic Improvement, Guangxi Botanical Garden of Medicinal Plants, Nanning, Guangxi 530023, PR China

[Jiang, Xing] Hunan Provincial Key Laboratory of Basic and Clinical Pharmacological Research of Gastrointestinal Cancer, Department of Pharmacy, lnstitute of Pharmacy and Pharmacology, the Second Affiliated Hospital, University of South China, Hengyang, Hunan 421001, PR China

[Tang, Guotao] Institute of Pharmacy and Pharmacology, Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hengyang Medical School, University of South China, Hengyang, Hunan 421001, PR China

[Quan, Haiyan] Hunan Polytechnic of Environment and Biology, Hengyang, Hunan 421001, PR China

[Wu, Fangfang] Engineering Research Center of Innovative Traditional Chinese, Zhuang and Yao Materia Medica, Ministry of Education, Guangxi University of Chinese Medicine, Nanning, Guangxi 530001, PR China. Electronic address: wffttn@163.com

通讯机构：

[Yang, Xiaonan] N

[Wu, Fangfang] E

Engineering Research Center of Innovative Traditional Chinese, Zhuang and Yao Materia Medica, Ministry of Education, Guangxi University of Chinese Medicine, Nanning, Guangxi 530001, PR China. Electronic address:

National Engineering Research Center for Southwest Endangered Medicinal Resources Development, Guangxi Key Laboratory of Medicinal Resources Protection and Genetic Improvement, Guangxi Botanical Garden of Medicinal Plants, Nanning, Guangxi 530023, PR China. Electronic address:

语种：

英文

关键词：

ACKR3;Hepatocellular carcinoma;Invasion;Migration;Proliferation;Scutellarein derivative TBS6b;Ubiquitination

期刊：

Bioorganic Chemistry

ISSN：

0045-2068

年：

2025

卷：

166

页码：

109073

DOI：

10.1016/j.bioorg.2025.109073

基金类别：

CRediT authorship contribution statement Xing Jiang: Writing – review & editing, acquisition, Formal analysis. Ying Liang: Writing – review & editing, acquisition, Formal analysis. Guotao Tang: Resources, Investigation. Haiyan Quan: Writing – original draft, Validation. Lijun Ruan: Investigation. Mengli Zhang: Investigation. Zhijun Song: Investigation. Min Ou: Investigation. Zhien Tan: Investigation. Fangfang Wu: Writing – review & editing, acquisition, Formal analysis. Xiaonan Yang: Writing – review & editing, This work was supported by the grant from the National Science and Technology Fundamental Resources Investigation Program of China (No. 2018FY100700 ), Guangxi Natural Science Foundation Program ( 2023GXNSFBA026354 ), the Program of Natural Science Foundation of China ( 82360767 , 82260747 , 82060689 ), Agriculture Research System of China of MOF and MARA ( CARS-21 ), Guangxi Key Laboratory of Medicinal Resources Protection and Genetic Improvement ( KL2022ZZ01 ) and National Key Research and Development

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本校为其他机构

院系归属：

药学与生物科学学院

摘要：

Scutellarein, a flavonoid compound from the traditional Chinese herb Scutellaria baicalensis , exhibits inhibitory effects against hepatocellular carcinoma (HCC), but its clinical application is limited by relatively weak potency. To enhance its antitumor activity, we synthesized a novel derivative, 5,6,7-trimethoxy-4′-benzimidazolyl scutellarein 6b (TBS6b), by introducing antitumor pharmacophores—trimethoxyphenyl and benzimidazole—into the scutellarein scaffold. TBS6b demonstrated significantly improved anti-HCC activity both in vitro and i...

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Binding and ubiquitination-mediated degradation of ACKR3 by the novel Scutellarein derivative TBS6b potently suppresses hepatocellular carcinoma

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