The discovery of a novel series of potential ERR alpha inverse agonists based on p-nitrobenzenesulfonamide template for triple-negative breast cancer in vivo
文献类型：期刊论文
| 作者 | Gao, Zhipei1; Wang, Tianxiao2; Li, Rui1; Du, Yongli1; Lv, Han1; Zhang, Liudi2; Chen, Haifei2; Shi, Xiaojin2; Li, Qunyi2; Shen, Jingkang3 |
| 刊名 | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
 |
| 出版日期 | 2022 |
| 卷号 | 37期号:1页码:125-134 |
| 关键词 | ERR alpha TNBC p-Nitrobenzenesulfonamide inverse agonist |
| ISSN号 | 1475-6366 |
| DOI | 10.1080/14756366.2021.1995728 |
| 通讯作者 | Du, Yongli(ylduyjs2019@163.com) ; Li, Qunyi(qyli1234@163.com) |
| 英文摘要 | Oestrogen related receptor alpha participated in the regulation of oxidative metabolism and mitochondrial biogenesis, and was overexpressed in many cancers including triple-negative breast cancer. A set of new ERR alpha inverse agonists based on p-nitrobenzenesulfonamide template were discovered and compound 11 with high potent activity (IC50 = 0.80 mu M) could significantly inhibit the transcription of ERR alpha-regulated target genes. By regulating the downstream signalling pathway, compound 11 could suppress the migration and invasion of the ER-negative MDA-MB-231 cell line. Furthermore, compound 11 demonstrated a significant growth suppression of breast cancer xenograft tumours in vivo (inhibition rate 23.58%). The docking results showed that compound 11 could form hydrogen bonds with Glu331 and Arg372 in addition to its hydrophobic interaction with ligand-binding domain. Our data implied that compound 11 represented a novel and effective ERR alpha inverse agonist, which had broad application prospects in the treatment of triple-negative breast cancer. |
| WOS关键词 | ESTROGEN-RELATED RECEPTOR ; CRYSTAL-STRUCTURE ; SURVIVAL ; IDENTIFICATION ; EXPRESSION ; COMPLEX ; GROWTH ; CELLS |
| 资助项目 | National Natural Science Foundation of China[81872744] ; National Natural Science Foundation of China[81973399] ; National Natural Science Foundation of China[81901399] ; Shandong Provincial Natural Science Foundation[ZR2019MH046] ; Shanghai Health Commission Youth Fund Projects[20184Y0194] ; Shanghai Health Commission Youth Fund Projects[20204Y0445] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000729295100001 |
| 出版者 | TAYLOR & FRANCIS LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/299223]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Du, Yongli; Li, Qunyi |
| 作者单位 | 1.Qilu Univ Technol, Sch Chem & Chem Engn, Shandong Acad Sci, 3501 Da Xue Rd, Jinan 250353, Peoples R China 2.Fudan Univ, Huashan Hosp, Dept Pharm, Shanghai 200040, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai, Peoples R China |
| 推荐引用方式 GB/T 7714 | Gao, Zhipei,Wang, Tianxiao,Li, Rui,et al. The discovery of a novel series of potential ERR alpha inverse agonists based on p-nitrobenzenesulfonamide template for triple-negative breast cancer in vivo[J]. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY,2022,37(1):125-134. |
| APA | Gao, Zhipei.,Wang, Tianxiao.,Li, Rui.,Du, Yongli.,Lv, Han.,...&Shen, Jingkang.(2022).The discovery of a novel series of potential ERR alpha inverse agonists based on p-nitrobenzenesulfonamide template for triple-negative breast cancer in vivo.JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY,37(1),125-134. |
| MLA | Gao, Zhipei,et al."The discovery of a novel series of potential ERR alpha inverse agonists based on p-nitrobenzenesulfonamide template for triple-negative breast cancer in vivo".JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY 37.1(2022):125-134. |
入库方式： OAI收割
来源：上海药物研究所
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