Synthesis and Biological Evaluation of β-Lactam Derivatives Targeting Speckle-Type POZ Protein (SPOP)
文献类型：期刊论文
| 作者 | Zhou, Chenmao5; Hao, Xinyue5; Chen, Zhengyang1,2; Zhang, Runze1,2; Zhou, Qian1,5; Fan, Zisheng1,3,4; Zheng, Mingyue1,2,5 ; Hou, Hui1,2; Zhang, Sulin1,2; Guo, Hao6
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| 刊名 | ACS MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2024-01-25 |
| 卷号 | 15期号:2页码:270-279 |
| ISSN号 | 1948-5875 |
| 关键词 | Speckle-type POZ protein (SPOP) SPOP inhibitors Clear cell renal cell carcinoma (ccRCC) Structure-activityrelationship (SAR) |
| DOI | 10.1021/acsmedchemlett.3c00515 |
| 通讯作者 | Hou, Hui(houhui@simm.ac.cn) ; Zhang, Sulin(slzhang@simm.ac.cn) ; Guo, Hao(hao.guo@birdotech.com) |
| 英文摘要 | Speckle-type POZ protein (SPOP) acts as a cullin3-RING ubiquitin ligase adaptor, which facilitates the recognition and ubiquitination of substrate proteins. Previous research suggests that targeting SPOP holds promise in the treatment of clear cell renal cell carcinoma (ccRCC). On the basis of the reported SPOP inhibitor 230D7, a series of beta-lactam derivatives were synthesized in this study. The biological activity assessment of these compounds revealed E1 as the most potent inhibitor, which can disrupt the SPOP-substrate interactions in vitro and suppress the colony formation of ccRCC cells. Taken together, this study provided compound E1 as a potent inhibitor against ccRCC and offered insight into the development of the beta-lactam SPOP inhibitor. |
| WOS关键词 | RENAL-CELL CARCINOMA ; PATHWAY ; ADAPTER ; CANCER ; RESISTANCE ; SUNITINIB ; TUMORS |
| 资助项目 | Shanghai Sailing Program[21YF1455900] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| 出版者 | AMER CHEMICAL SOC |
| WOS记录号 | WOS:001160628000001 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/309240]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Hou, Hui; Zhang, Sulin; Guo, Hao |
| 作者单位 | 1.Chinese Acad Sci, Drug Discovery & Design Ctr, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.ShanghaiTech Univ, Shanghai Inst Adv Immunochem Studies, Shanghai 201210, Peoples R China 4.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 201210, Peoples R China 5.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China 6.Birdo Shanghai Pharmatech Co Ltd, Shanghai 201318, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhou, Chenmao,Hao, Xinyue,Chen, Zhengyang,et al. Synthesis and Biological Evaluation of β-Lactam Derivatives Targeting Speckle-Type POZ Protein (SPOP)[J]. ACS MEDICINAL CHEMISTRY LETTERS,2024,15(2):270-279. |
| APA | Zhou, Chenmao.,Hao, Xinyue.,Chen, Zhengyang.,Zhang, Runze.,Zhou, Qian.,...&Guo, Hao.(2024).Synthesis and Biological Evaluation of β-Lactam Derivatives Targeting Speckle-Type POZ Protein (SPOP).ACS MEDICINAL CHEMISTRY LETTERS,15(2),270-279. |
| MLA | Zhou, Chenmao,et al."Synthesis and Biological Evaluation of β-Lactam Derivatives Targeting Speckle-Type POZ Protein (SPOP)".ACS MEDICINAL CHEMISTRY LETTERS 15.2(2024):270-279. |
入库方式： OAI收割
来源：上海药物研究所
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