ShanghaiTech University Knowledge Management System
| Synthesis and Biological Evaluation of β‐Lactam Derivatives Targeting Speckle-Type POZ Protein (SPOP) | |
| 2024-01 | |
| 发表期刊 | ACS MEDICINAL CHEMISTRY LETTERS (IF:3.5[JCR-2023],3.9[5-Year]) |
| ISSN | 1948-5875 |
| 发表状态 | 已发表 |
| DOI | 10.1021/acsmedchemlett.3c00515 |
| 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 β-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 β-lactam SPOP inhibitor. |
| 关键词 | Speckle-type POZ protein (SPOP) SPOP inhibitors Clear cell renal cell carcinoma (ccRCC) Structure−activity relationship (SAR) |
| 学科门类 | 理学::化学 ; 理学::生物学 ; 医学::药学（可授医学、理学学位） |
| URL | 查看原文 |
| 文献类型 | 期刊论文 |
| 条目标识符 | https://kms.shanghaitech.edu.cn/handle/2MSLDSTB/449044 |
| 专题 | 免疫化学研究所 生命科学与技术学院_博士生 |
| 共同第一作者 | Xinyue Hao; Zhengyang Chen |
| 作者单位 | 1.School of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing 210023, China 2.Drug Discovery and Design Center, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China 3.University of Chinese Academy of Sciences, Beijing 100049, China 4.Shanghai Institute for Advanced Immunochemical Studies and School of Life Science and Technology, ShanghaiTech University, Shanghai 201210, China |
| 推荐引用方式 GB/T 7714 | Chenmao Zhou,Xinyue Hao,Zhengyang Chen,et al. Synthesis and Biological Evaluation of β‐Lactam Derivatives Targeting Speckle-Type POZ Protein (SPOP)[J]. ACS MEDICINAL CHEMISTRY LETTERS,2024. |
| APA | Chenmao Zhou.,Xinyue Hao.,Zhengyang Chen.,Runze Zhang.,Qian Zhou.,...&Hao Guo.(2024).Synthesis and Biological Evaluation of β‐Lactam Derivatives Targeting Speckle-Type POZ Protein (SPOP).ACS MEDICINAL CHEMISTRY LETTERS. |
| MLA | Chenmao Zhou,et al."Synthesis and Biological Evaluation of β‐Lactam Derivatives Targeting Speckle-Type POZ Protein (SPOP)".ACS MEDICINAL CHEMISTRY LETTERS (2024). |
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