Jianling Long , Pengju Ye , Weixi Yuan , Qixian Yang , Zhe Wang , Hongxiang Xiao , Zhizhong Xie , Xiaoyong Lei , Xiaoyan Yang , Xiangping Deng , Guotao Tang
{"title":"黄酮类化合物靶向雌激素受体治疗乳腺癌的研究进展","authors":"Jianling Long , Pengju Ye , Weixi Yuan , Qixian Yang , Zhe Wang , Hongxiang Xiao , Zhizhong Xie , Xiaoyong Lei , Xiaoyan Yang , Xiangping Deng , Guotao Tang","doi":"10.1016/j.bmc.2025.118106","DOIUrl":null,"url":null,"abstract":"<div><div>Breast cancer (BC) stands as the most prevalent malignancy among women. Targeting the estrogen receptor (ER) or ER pathway is one of the important approaches for ER<sup>+</sup> BC treatment. As a class of phytoestrogens, flavonoids possess notable anti-tumor properties and hold immense potential in regulating ER signaling. In this review, we reported the recent advances in both <em>in vitro</em> and <em>in vivo</em> studies of flavonoids and their synthetic derivatives targeting the ER signaling pathway, including the target and mechanism of action of these molecules, as well as their structure–activity relationship. Based on the available literature, the beneficial effects of flavonoids as ER targeting agents are promising but they require further <em>in vitro</em> and <em>in vivo</em> studies to enable its translation from bench to bedside. This review will provide valuable guidance and insights for the future development of drugs targeting the ER pathway.</div></div>","PeriodicalId":255,"journal":{"name":"Bioorganic & Medicinal Chemistry","volume":"120 ","pages":"Article 118106"},"PeriodicalIF":3.3000,"publicationDate":"2025-02-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Research progress of flavonoids targeting estrogen receptor in the treatment of breast cancer\",\"authors\":\"Jianling Long , Pengju Ye , Weixi Yuan , Qixian Yang , Zhe Wang , Hongxiang Xiao , Zhizhong Xie , Xiaoyong Lei , Xiaoyan Yang , Xiangping Deng , Guotao Tang\",\"doi\":\"10.1016/j.bmc.2025.118106\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>Breast cancer (BC) stands as the most prevalent malignancy among women. Targeting the estrogen receptor (ER) or ER pathway is one of the important approaches for ER<sup>+</sup> BC treatment. As a class of phytoestrogens, flavonoids possess notable anti-tumor properties and hold immense potential in regulating ER signaling. In this review, we reported the recent advances in both <em>in vitro</em> and <em>in vivo</em> studies of flavonoids and their synthetic derivatives targeting the ER signaling pathway, including the target and mechanism of action of these molecules, as well as their structure–activity relationship. Based on the available literature, the beneficial effects of flavonoids as ER targeting agents are promising but they require further <em>in vitro</em> and <em>in vivo</em> studies to enable its translation from bench to bedside. This review will provide valuable guidance and insights for the future development of drugs targeting the ER pathway.</div></div>\",\"PeriodicalId\":255,\"journal\":{\"name\":\"Bioorganic & Medicinal Chemistry\",\"volume\":\"120 \",\"pages\":\"Article 118106\"},\"PeriodicalIF\":3.3000,\"publicationDate\":\"2025-02-07\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Bioorganic & Medicinal Chemistry\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0968089625000471\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"BIOCHEMISTRY & MOLECULAR BIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Bioorganic & Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0968089625000471","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
Research progress of flavonoids targeting estrogen receptor in the treatment of breast cancer
Breast cancer (BC) stands as the most prevalent malignancy among women. Targeting the estrogen receptor (ER) or ER pathway is one of the important approaches for ER+ BC treatment. As a class of phytoestrogens, flavonoids possess notable anti-tumor properties and hold immense potential in regulating ER signaling. In this review, we reported the recent advances in both in vitro and in vivo studies of flavonoids and their synthetic derivatives targeting the ER signaling pathway, including the target and mechanism of action of these molecules, as well as their structure–activity relationship. Based on the available literature, the beneficial effects of flavonoids as ER targeting agents are promising but they require further in vitro and in vivo studies to enable its translation from bench to bedside. This review will provide valuable guidance and insights for the future development of drugs targeting the ER pathway.
期刊介绍:
Bioorganic & Medicinal Chemistry provides an international forum for the publication of full original research papers and critical reviews on molecular interactions in key biological targets such as receptors, channels, enzymes, nucleotides, lipids and saccharides.
The aim of the journal is to promote a better understanding at the molecular level of life processes, and living organisms, as well as the interaction of these with chemical agents. A special feature will be that colour illustrations will be reproduced at no charge to the author, provided that the Editor agrees that colour is essential to the information content of the illustration in question.