A heterobifunctional molecule recruits cereblon to an RNA scaffold and activates its PROTAC function
文献类型：期刊论文
| 作者 | Xu, Yan2,5; Fu, Dingqiang2,3; Yuan, Yi3; Peng, Yan2,3; Dong, Juan3; Du, Feng3; Huang, Xin3; Li, Guangxun3; Chen, Xiaohua1 ; Wang, Qiwei4,5
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| 刊名 | CELL REPORTS PHYSICAL SCIENCE
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| 出版日期 | 2022-10-19 |
| 卷号 | 3期号:10页码:12 |
| DOI | 10.1016/j.xcrp.2022.101064 |
| 通讯作者 | Chen, Xiaohua(xhchen@simm.ac.cn) ; Wang, Qiwei(wqw@cioc.ac.cn) ; Tang, Zhuo(tangzhuo@cib.ac.cn) |
| 英文摘要 | The ability to regulate protein abundance provides huge opportunities for the development of treatments for various diseases. The proteolysis-targeting chimera (PROTAC) provides powerful tools to degrade these undruggable targets, becoming a promising technology. Herein, we report the development of aptamer-based PROTACs as a novel strategy to broaden the spectrum of targets. The RNA aptamer of the target protein applied in targeted degradation. A heterobifunctional molecule can recruit E3 ubiquitin ligase to a genetically encoded tandem aptamer RNA scaffold, promoting ubiquitination and degradation of target proteins. Partial degradations of different target proteins, including p50, p65, and E2F1, have been achieved by simply replacing the 3' module on the RNA scaffold with the corresponding RNA aptamers. Besides, simultaneous degradation of multiple target proteins is realized through inserting more aptamer into RNA scaffold. Thus, the aptamer-based PROTAC technology offers a general strategy for targeted protein degradation in drug discovery and biological research. |
| WOS关键词 | NF-KAPPA-B ; GREEN FLUORESCENT PROTEIN ; CANCER ; DEGRADATION ; CHALLENGES ; GENERATION ; SELECTION ; APTAMERS ; FAMILY ; ROLES |
| 资助项目 | National Natural Science Foundation of China[22177111] ; National Natural Science Foundation of China[21907090] ; National Natural Science Foundation of China[21877108] ; Sichuan Science and Technology Program[2019ZDZX0048] ; Sichuan Science and Technology Program[2020YFS0370] ; Sichuan Medical Research Program[S20005] ; Chengdu Municipal Bureau of Science and Technology[2021-YF05-01739-SN] ; Youth Innovation Promotion Association CAS[2020365] |
| WOS研究方向 | Chemistry ; Energy & Fuels ; Materials Science ; Physics |
| 语种 | 英语 |
| 出版者 | ELSEVIER |
| WOS记录号 | WOS:000907255000011 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/303887]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Chen, Xiaohua; Wang, Qiwei; Tang, Zhuo |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China 2.Univ Chinese Acad Sci, Beijing 10049, Peoples R China 3.Chinese Acad Sci, Chengdu Inst Biol, Nat Prod Res Ctr, Chengdu 610041, Sichuan, Peoples R China 4.Xihua Univ, Dept Chem, Chengdu 610039, Peoples R China 5.Chinese Acad Sci, Chengdu Inst Organ Chem, Chengdu 610041, Sichuan, Peoples R China |
| 推荐引用方式 GB/T 7714 | Xu, Yan,Fu, Dingqiang,Yuan, Yi,et al. A heterobifunctional molecule recruits cereblon to an RNA scaffold and activates its PROTAC function[J]. CELL REPORTS PHYSICAL SCIENCE,2022,3(10):12. |
| APA | Xu, Yan.,Fu, Dingqiang.,Yuan, Yi.,Peng, Yan.,Dong, Juan.,...&Tang, Zhuo.(2022).A heterobifunctional molecule recruits cereblon to an RNA scaffold and activates its PROTAC function.CELL REPORTS PHYSICAL SCIENCE,3(10),12. |
| MLA | Xu, Yan,et al."A heterobifunctional molecule recruits cereblon to an RNA scaffold and activates its PROTAC function".CELL REPORTS PHYSICAL SCIENCE 3.10(2022):12. |
入库方式： OAI收割
来源：上海药物研究所
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