Construction of PROTAC Library via Liquid-Phase Synthesis Enabled by a Hydrophobic Tag
文献类型：期刊论文
| 作者 | Zhou, Yifeng1,2; He, Wei4; Zhou, Zehui1,2; Wu, Min4; Wu, Qianping1,2,3; Tao, Zhaofan1,2; Zheng, Mingyue1,3,4; Zhang, Sulin1,3,4; Xu, Tianfeng1,2,3 |
| 刊名 | ORGANIC LETTERS
 |
| 出版日期 | 2026-02-27 |
| 卷号 | 28期号:8页码:2747-2752 |
| ISSN号 | 1523-7060 |
| DOI | 10.1021/acs.orglett.6c00263 |
| 英文摘要 | Herein, we present a new synthetic strategy for PROTAC development by using hydrophobic tag-assisted liquid-phase synthesis (LPS). The hydrophobic tag enables intermediates to be purified by precipitation, thus sparing the effort of column purification. Adopting this strategy, we efficiently constructed highly diverse linker and androgen receptor (AR)-targeting PROTAC libraries. Among the 26 synthesized PROTACs, compound 25 emerged as the most potent one, exhibiting a subnanomolar DC50 value, high D max, and strong antiproliferative activity. |
| 资助项目 | National Natural Science Foundation of China[22107110] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:001690703700001 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/322996]  |
| 专题 | 国家级研究中心_原创新药研究全国重点实验室 |
| 通讯作者 | Zhang, Sulin; Xu, Tianfeng |
| 作者单位 | 1.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, Shanghai 201203, Peoples R China 3.Univ Chinese Acad Sci, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 310024, Peoples R China 4.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhou, Yifeng,He, Wei,Zhou, Zehui,et al. Construction of PROTAC Library via Liquid-Phase Synthesis Enabled by a Hydrophobic Tag[J]. ORGANIC LETTERS,2026,28(8):2747-2752. |
| APA | Zhou, Yifeng.,He, Wei.,Zhou, Zehui.,Wu, Min.,Wu, Qianping.,...&Xu, Tianfeng.(2026).Construction of PROTAC Library via Liquid-Phase Synthesis Enabled by a Hydrophobic Tag.ORGANIC LETTERS,28(8),2747-2752. |
| MLA | Zhou, Yifeng,et al."Construction of PROTAC Library via Liquid-Phase Synthesis Enabled by a Hydrophobic Tag".ORGANIC LETTERS 28.8(2026):2747-2752. |
入库方式： OAI收割
来源：上海药物研究所
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