中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
首页 机构 成果 学者
  
  1. CAS IR Grid
  2. 上海药物研究所
  3. 中国科学院上海药物研究所
A Versatile Bioorthogonal Theranostic Platform Enables Relay Activation of Tumor Cell Imaging and Targeted Protein Degradation

文献类型：期刊论文

作者Sun, Feilong5; Wang, Tian1; Wang, Pengfei3,4; Shi, Jiaxin1; Shen, Yanyan4; Wang, Guilong2; Yang, Biyu4; Li, Huiwen3,5; Zhang, Qiumeng5; Chen, Yi3,4
刊名JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
出版日期2025-11-28
页码11
ISSN号0002-7863
DOI10.1021/jacs.5c11564
通讯作者Zhang, Qiumeng(qmzhang@simm.ac.cn) ; Chen, Yi(ychen@simm.ac.cn) ; Zhang, Xuan(zhangxuan@simm.ac.cn)
英文摘要Targeted protein degradation offers therapeutic promise but often suffers from on-target off-tissue toxicities. To overcome this challenge, we developed a versatile theranostic platform that integrates tumor cell imaging with precisely controlled protein degradation. Central to this platform is XZ2223, a glutathione (GSH)-cleavable bioorthogonal trigger that couples cancer cell labeling with concomitant tetrazine release, thereby activating trans-cyclooctene (TCO)-caged CRBN-recruiting degrader prodrugs, Pro-CC-885 and Pro-dBET6, to induce on-demand degradation of GSPT1 and BET, respectively. Coadministration of XZ2223 with either prodrug afforded robust tumor imaging and efficient protein degradation in xenograft models, while the XZ2223/Pro-dBET6 combination further elicited in vivo antitumor efficacy with reduced systemic toxicity. This innovative platform shows potential as a dual-function approach for precision cancer therapy.
WOS关键词PROTAC
资助项目Chinese Academy of Sciences[XDB1060401] ; National Natural Science Foundation of China[22277131] ; Pioneer Hundred Talents Program of the Chinese Academy of Sciences[NA]
WOS研究方向Chemistry
语种英语
WOS记录号WOS:001627228100001
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/322052]  
专题中国科学院上海药物研究所
通讯作者Zhang, Qiumeng; Chen, Yi; Zhang, Xuan
作者单位1.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China
2.Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, Shenyang 110016, Peoples R China
3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Chem Biol, Shanghai 201203, Peoples R China
5.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Dev Ctr, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Sun, Feilong,Wang, Tian,Wang, Pengfei,et al. A Versatile Bioorthogonal Theranostic Platform Enables Relay Activation of Tumor Cell Imaging and Targeted Protein Degradation[J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY,2025:11.
APA Sun, Feilong.,Wang, Tian.,Wang, Pengfei.,Shi, Jiaxin.,Shen, Yanyan.,...&Zhang, Xuan.(2025).A Versatile Bioorthogonal Theranostic Platform Enables Relay Activation of Tumor Cell Imaging and Targeted Protein Degradation.JOURNAL OF THE AMERICAN CHEMICAL SOCIETY,11.
MLA Sun, Feilong,et al."A Versatile Bioorthogonal Theranostic Platform Enables Relay Activation of Tumor Cell Imaging and Targeted Protein Degradation".JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2025):11.

入库方式： OAI收割

来源：上海药物研究所

浏览0
下载0
收藏0
其他版本

除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。