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Programmable Repurposing of Existing Drugs as Pharmaceutical Elements for the Construction of Aptamer-Drug Conjugates

文献类型：期刊论文

作者Gao, Fei1,2,4; Zhou, Jinming3; Sun, Yang1,4; Yang, Cai1,4; Zhang, Shiyan1,4; Wang, Ruowen1,4; Tan, Weihong1,4,5
刊名ACS APPLIED MATERIALS & INTERFACES
出版日期2021-03-03
卷号13
ISSN号1944-8244
关键词aptamer pharmaceutical elements solid-phase synthesis targeted therapy drug delivery
DOI10.1021/acsami.0c18846
通讯作者Wang, Ruowen(wangwrw@sjtu.edu.cn) ; Tan, Weihong(tan@hnu.edu.cn)
英文摘要Converting marketed drug molecules into phos-phoramidites may present a potential strategy to facilitate the development of aptamer-drug conjugates (ApDCs) by a DNA synthesizer in a programmable way; however, quite limited methods were reported. Herein, we demonstrated a general approach by repurposing camptothecin (CPT) species. Commonly used inactive ingredients in pharmaceuticals are investigated and selected as a bonding moiety, from which 2-mercaptoethoxy ethanol and thioglycerol were efficiently incorporated with CPT to give the precursors. Cell viability and molecular docking results of the precursors supported that incorporation of the bonding moiety would not interrupt the inhibitory activity. Therefore, corresponding phosphoramidites were prepared as pharmaceutical elements, and a series of ApDCs were constructed automatically by solid-phase synthesis. Biological studies revealed that CPT elements could be specifically delivered to HCT116 cells by an aptamer and released inside cells. This kind of programmable repurposing may take advantage of established safety data and efficacy of existing drugs resulting in a faster development of ApDCs.
资助项目National Science Foundation of China[21877079] ; National Science Foundation of China[81803068]
WOS研究方向Science & Technology - Other Topics ; Materials Science
语种英语
出版者AMER CHEMICAL SOC
WOS记录号WOS:000626502700022
资助机构National Science Foundation of China
源URL[http://ir.hfcas.ac.cn:8080/handle/334002/121086]  
专题中国科学院合肥物质科学研究院
通讯作者Wang, Ruowen; Tan, Weihong
作者单位1.Shanghai Jiao Tong Univ, Coll Chem & Chem Engn, Shanghai 200240, Peoples R China
2.Shanghai Univ, Inst Translat Med, Shanghai 200444, Peoples R China
3.Zhejiang Normal Univ, Dept Chem, Key Lab, Minist Educ Adv Catalysis Mat, 688 Yingbin Rd, Jinhua 321004, Zhejiang, Peoples R China
4.Shanghai Jiao Tong Univ, Inst Mol Med IMM, State Key Lab Oncogenes & Related Genes, Renji Hosp,Sch Med, Shanghai 200240, Peoples R China
5.Univ Chinese Acad Sci, Chinese Acad Sci, Inst Basic Med & Canc IBMC, Canc Hosp, Hangzhou 310022, Zhejiang, Peoples R China
推荐引用方式
GB/T 7714		 Gao, Fei,Zhou, Jinming,Sun, Yang,et al. Programmable Repurposing of Existing Drugs as Pharmaceutical Elements for the Construction of Aptamer-Drug Conjugates[J]. ACS APPLIED MATERIALS & INTERFACES,2021,13.
APA Gao, Fei.,Zhou, Jinming.,Sun, Yang.,Yang, Cai.,Zhang, Shiyan.,...&Tan, Weihong.(2021).Programmable Repurposing of Existing Drugs as Pharmaceutical Elements for the Construction of Aptamer-Drug Conjugates.ACS APPLIED MATERIALS & INTERFACES,13.
MLA Gao, Fei,et al."Programmable Repurposing of Existing Drugs as Pharmaceutical Elements for the Construction of Aptamer-Drug Conjugates".ACS APPLIED MATERIALS & INTERFACES 13(2021).

入库方式： OAI收割

来源：合肥物质科学研究院

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