Evidence mapPaperPMID 40091020Full record

ArticleJournal of biomedical science2025

Metformin sensitizes triple-negative breast cancer to histone deacetylase inhibitors by targeting FGFR4.

Zhangyuan Gu, Fugui Ye, Hong Luo, Xiaoguang Li, Yue Gong, Shiqi Mao, Xiaoqing Jia, Xiangchen Han, Boyue Han, Yun Fu and 6 more

Abstract read
In one paragraph

Article in Journal of biomedical science, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

7 citing papers in PubMed.

  1. Article
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

16 authors.

Zhangyuan Gu *Department of Breast Surgery, Shanghai Key Laboratory of Maternal-Fetal Medicine, Shanghai Institute of Maternal-Fetal Medicine and Gynecologic Oncology, Shanghai First Maternity and Infant Hospital, School of Medicine, Tongji University, No. 2699 West Gao-Ke Road, Shanghai, 201204, China.
Fugui Ye *Department of Breast Surgery, Key Laboratory of Breast Cancer in Shanghai, Fudan University Shanghai Cancer Center, No.688 Hong-Qu Road, Shanghai, 200032, China.
Hong Luo *Department of Breast Surgery, Key Laboratory of Breast Cancer in Shanghai, Fudan University Shanghai Cancer Center, No.688 Hong-Qu Road, Shanghai, 200032, China.
Xiaoguang LiShanghai Henlius Biotech Inc., Shanghai, 200233, China.
Yue GongDepartment of Breast Surgery, Key Laboratory of Breast Cancer in Shanghai, Fudan University Shanghai Cancer Center, No.688 Hong-Qu Road, Shanghai, 200032, China.
Shiqi MaoDepartment of Medical Oncology, Shanghai Pulmonary Hospital, Cancer Institute, Tongji University School of Medicine, Shanghai, 200433, China.
Xiaoqing JiaDepartment of Breast Surgery, Shanghai Key Laboratory of Maternal-Fetal Medicine, Shanghai Institute of Maternal-Fetal Medicine and Gynecologic Oncology, Shanghai First Maternity and Infant Hospital, School of Medicine, Tongji University, No. 2699 West Gao-Ke Road, Shanghai, 201204, China.
Xiangchen HanDepartment of Breast Surgery, Key Laboratory of Breast Cancer in Shanghai, Fudan University Shanghai Cancer Center, No.688 Hong-Qu Road, Shanghai, 200032, China.
Boyue HanDepartment of Breast Surgery, Key Laboratory of Breast Cancer in Shanghai, Fudan University Shanghai Cancer Center, No.688 Hong-Qu Road, Shanghai, 200032, China.
Yun FuDepartment of Breast Surgery, Shanghai Key Laboratory of Maternal-Fetal Medicine, Shanghai Institute of Maternal-Fetal Medicine and Gynecologic Oncology, Shanghai First Maternity and Infant Hospital, School of Medicine, Tongji University, No. 2699 West Gao-Ke Road, Shanghai, 201204, China.
Xiaolin ChengDepartment of Breast Surgery, Shanghai Key Laboratory of Maternal-Fetal Medicine, Shanghai Institute of Maternal-Fetal Medicine and Gynecologic Oncology, Shanghai First Maternity and Infant Hospital, School of Medicine, Tongji University, No. 2699 West Gao-Ke Road, Shanghai, 201204, China.
Jiejing LiDepartment of Breast Surgery, Shanghai Key Laboratory of Maternal-Fetal Medicine, Shanghai Institute of Maternal-Fetal Medicine and Gynecologic Oncology, Shanghai First Maternity and Infant Hospital, School of Medicine, Tongji University, No. 2699 West Gao-Ke Road, Shanghai, 201204, China.
Zhiming ShaoDepartment of Breast Surgery, Key Laboratory of Breast Cancer in Shanghai, Fudan University Shanghai Cancer Center, No.688 Hong-Qu Road, Shanghai, 200032, China. zhi_ming_shao@163.com.
Peizhen WenDepartment of General Surgery, School of Medicine, Organ Transplantation Clinical Medical Center of Xiamen University, Xiang'an Hospital of Xiamen University, Xiamen University, No. 2000 Xiang'an East Road, Xiamen, 361005, Fujian, China. wenpeizhen1996@163.com.
Xin HuDepartment of Breast Surgery, Key Laboratory of Breast Cancer in Shanghai, Fudan University Shanghai Cancer Center, No.688 Hong-Qu Road, Shanghai, 200032, China. xinhu@fudan.edu.cn.
Zhigang ZhuangDepartment of Breast Surgery, Shanghai Key Laboratory of Maternal-Fetal Medicine, Shanghai Institute of Maternal-Fetal Medicine and Gynecologic Oncology, Shanghai First Maternity and Infant Hospital, School of Medicine, Tongji University, No. 2699 West Gao-Ke Road, Shanghai, 201204, China. zhuangzhigang1971@163.com.

Funding

Pudong New Area Gynaecology and Obstetrics Medical Treatment Combination Project PDYLT2022-05the Ministry of Science and Technology Fund MOST2016YFC0900300the National Natural Science Foundation of China Youth Science Foundation Project 82002798the National Natural Science Foundation of China Youth Science Foundation Project 82102944the Shanghai Committee of Science and Technology Funds 14ZR1429600the Shanghai Committee of Science and Technology Funds 15410724000the Shanghai Committee of Science and Technology Funds 15411953300the Shanghai Committee of Science and Technology Funds 21ZR1451000the Shanghai Municipal Health Commission Project 20204Y0131the Shanghai Municipal Health Commission Project 20214Y0255
6 · The paper itself

Abstract

backgroundTriple-negative breast cancer (TNBC) is characterized by high malignancy, strong invasiveness, and a propensity for distant metastasis, leading to poor prognosis and relatively limited treatment options. Metformin, as a first-line oral hypoglycemic agent, has garnered widespread research interest in recent years due to its potential in cancer prevention and treatment. However, its efficacy varies significantly across different tumor types. Histone deacetylase inhibitors (HDACi), such as SAHA, have demonstrated antitumor activity, but TNBC responds poorly to HDACi monotherapy, possibly due to feedback activation of the JAK-STAT pathway. Exploring the synergistic potential and underlying mechanisms of combining metformin with HDACi in TNBC treatment is crucial.

methodsWe predicted the synergistic effects of metformin and SAHA in TNBC using multiple computational methods (CMap, DTsyn, and DrugComb). We also developed a cancer-specific compound mimic library (CDTSL) and applied a three-step strategy to identify genes fitting the "metformin sensitization" model. Subsequently, we evaluated the synergistic effects of metformin and SAHA in TNBC cell lines through cell proliferation, colony formation, and apoptosis assays. Furthermore, we investigated the molecular mechanisms of the combined treatment using techniques such as transcriptome sequencing, chromatin immunoprecipitation (ChIP), Western blotting, and measurement of extracellular acidification rate (ECAR). Additionally, we assessed the in vivo antitumor effects of the combined therapy in a nude mouse subcutaneous xenograft model.

resultsCMap, DTsyn, and DrugComb all predicted the synergistic effects of SAHA and metformin in TNBC. The screening results revealed that HDAC10 played a key role in metformin sensitization. We found that the combination of metformin and SAHA exhibited synergistic antitumor effects (combination index CI < 0.9) in TNBC cell lines. Mechanistically, metformin inhibited histone acetylation on FGFR4, thereby blocking the feedback activation of FGFR4 downstream pathways induced by SAHA. Furthermore, metformin interfered with the glycolysis process induced by SAHA, altering the metabolic reprogramming of tumor cells. In in vivo experiments, the combined treatment of metformin and SAHA significantly inhibited the growth of subcutaneous tumors in nude mice.

conclusionsMetformin enhances the sensitivity of TNBC to HDAC inhibitors by blocking the FGFR4 pathway and interfering with metabolic reprogramming. When used in combination with SAHA, metformin exhibits synergistic antitumor effects. Our study provides a theoretical basis for the combined application of HDAC inhibitors and metformin, potentially offering a new strategy for the treatment of TNBC.

Indexed as

Histone Deacetylase InhibitorsMetforminTriple Negative Breast NeoplasmsAnimalsCell Line, TumorDrug SynergismFemaleHumansMiceMice, NudeXenograft Model Antitumor AssaysHistone Deacetylase InhibitorsMetforminDrug synergismHistone deacetylase inhibitorsMetforminTriple-negative breast neoplasms

Identifiers

PMID40091020
PMCPMC11912690

What Socratic holds

Textmetadata
LicenceCC BY
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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.