Advances in Medicinal Chemistry of Estrogen-related Receptor Alpha (ERRa) Inverse Agonists
文献类型：期刊论文
| 作者 | Zhang, Haibin1; Du, Yongli1; Zheng, Yong1; Lv, Huiting1; Yan, Zhijia1; Dong, Ning1; Zhu, Yaling1; Shen, Jingkang2 |
| 刊名 | CURRENT TOPICS IN MEDICINAL CHEMISTRY
 |
| 出版日期 | 2023 |
| 卷号 | 23期号:20页码:1952-1963 |
| ISSN号 | 1568-0266 |
| 关键词 | ERRalpha ERRalpha inverse agonists Breast cancer TNBC Signaling pathways Inverse agonistic activity |
| DOI | 10.2174/1568026623666230515145822 |
| 通讯作者 | Du, Yongli(yldu2016@163.com) |
| 英文摘要 | Estrogen-related receptor alpha (ERR & alpha;), a member of the nuclear receptor superfamily, is strongly expressed in breast cancer cells. Its overexpression is associated with poor prognosis in triple-negative Breast Cancer (TNBC). ERR & alpha; expression could be inhibited by the downregulation of upstream oncogenic growth factors mTOR, HER2, and PI3K. Low expression of ERR & alpha; could suppress the migration and angiogenesis of tumor cells by inhibiting the activity of its downstream signals VEGF and WNT11. Studies have confirmed that ERR & alpha; inverse agonists can inhibit ERR & alpha; expression to treat breast cancer. Inverse agonists of ERR & alpha; could disrupt the interactions of ERR & alpha; with its coactivators and inhibit tumor development. Existing ERR & alpha; inverse agonists have shown moderate efficacy in inhibiting the growth of breast cancer cells. Clinical inverse agonists of ERR & alpha; have not been found in the literature. This review focuses on the research progress and the structure-activity relationship of ERR & alpha; inverse agonists, providing guidance for the research and discovery of new anti-tumor compounds for TNBC. |
| WOS关键词 | THERAPEUTIC TARGET ; CRYSTAL-STRUCTURE ; IN-VIVO ; GROWTH ; IDENTIFICATION ; DIFFERENTIATION ; ANGIOGENESIS ; METABOLISM ; EXPRESSION ; DISCOVERY |
| 资助项目 | Declared none. |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| 出版者 | BENTHAM SCIENCE PUBL LTD |
| WOS记录号 | WOS:001058535800004 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/306158]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Du, Yongli |
| 作者单位 | 1.Qilu Univ Technol, Shandong Acad Sci, Sch Chem & Chem Engn, 3501 Da Xue Rd, Jinan 250353, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Haibin,Du, Yongli,Zheng, Yong,et al. Advances in Medicinal Chemistry of Estrogen-related Receptor Alpha (ERRa) Inverse Agonists[J]. CURRENT TOPICS IN MEDICINAL CHEMISTRY,2023,23(20):1952-1963. |
| APA | Zhang, Haibin.,Du, Yongli.,Zheng, Yong.,Lv, Huiting.,Yan, Zhijia.,...&Shen, Jingkang.(2023).Advances in Medicinal Chemistry of Estrogen-related Receptor Alpha (ERRa) Inverse Agonists.CURRENT TOPICS IN MEDICINAL CHEMISTRY,23(20),1952-1963. |
| MLA | Zhang, Haibin,et al."Advances in Medicinal Chemistry of Estrogen-related Receptor Alpha (ERRa) Inverse Agonists".CURRENT TOPICS IN MEDICINAL CHEMISTRY 23.20(2023):1952-1963. |
入库方式： OAI收割
来源：上海药物研究所
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