Discovery Small-Molecule p300 Inhibitors Derived from a Newly Developed Indazolone-Focused DNA-Encoded Library
文献类型：期刊论文
| 作者 | Suo, Yanrui2,3; Li, Kaige1; Ling, Xing2,3; Yan, Kenian2,3; Lu, Weiwei3; Yue, Jinfeng3; Chen, Xiaohua2,3 ; Duan, Zhiqiang3; Lu, Xiaojie1,2,3
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| 刊名 | BIOCONJUGATE CHEMISTRY
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| 出版日期 | 2024-08-08 |
| 卷号 | 35期号:8页码:1251-1257 |
| ISSN号 | 1043-1802 |
| DOI | 10.1021/acs.bioconjchem.4c00307 |
| 通讯作者 | Chen, Xiaohua(xhchen@simm.ac.cn) ; Duan, Zhiqiang(duanzq@simm.ac.cn) ; Lu, Xiaojie(xjlu@simm.ac.cn) |
| 英文摘要 | The DNA-encoded library (DEL) is a robust tool for chemical biology and drug discovery. In this study, we developed a DNA-compatible light-promoted reaction that is highly efficient and plate-compatible for DEL construction based on the formation of the indazolone scaffold. Employing this high-efficiency approach, we constructed a DEL featuring an indazolone core, which enabled the identification of a novel series of ligands specifically targeting E1A-binding protein (p300) after DEL selection. Taken together, our findings underscore the feasibility of light-promoted reactions in DEL synthesis and unveil promising avenues for developing p300-targeting inhibitors. |
| WOS关键词 | ACETYLATION ; CHEMISTRY ; CBP/P300 |
| 资助项目 | National Natural Science Foundation of China (NSFC)[22377139] ; National Natural Science Foundation of China (NSFC)[92253305] ; National Natural Science Foundation of China (NSFC)[21907105] ; [SIMM0220233001] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:001287543300001 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/312712]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Chen, Xiaohua; Duan, Zhiqiang; Lu, Xiaojie |
| 作者单位 | 1.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Suo, Yanrui,Li, Kaige,Ling, Xing,et al. Discovery Small-Molecule p300 Inhibitors Derived from a Newly Developed Indazolone-Focused DNA-Encoded Library[J]. BIOCONJUGATE CHEMISTRY,2024,35(8):1251-1257. |
| APA | Suo, Yanrui.,Li, Kaige.,Ling, Xing.,Yan, Kenian.,Lu, Weiwei.,...&Lu, Xiaojie.(2024).Discovery Small-Molecule p300 Inhibitors Derived from a Newly Developed Indazolone-Focused DNA-Encoded Library.BIOCONJUGATE CHEMISTRY,35(8),1251-1257. |
| MLA | Suo, Yanrui,et al."Discovery Small-Molecule p300 Inhibitors Derived from a Newly Developed Indazolone-Focused DNA-Encoded Library".BIOCONJUGATE CHEMISTRY 35.8(2024):1251-1257. |
入库方式： OAI收割
来源：上海药物研究所
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