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Construction of Bispecific Aptamer-Drug Conjugate by a Hybrid Chemical and Biological Approach
Sun, Yang1,2; Gao, Fei1,2; Yang, Cai1,2; Li, Yingying3,4; Jin, Cheng3,4; Xie, Sitao3,4; Lv, Cheng1; Ding, Ding1; Han, Da1; Li, Juan1; Wang, Ruowen1,2; Tan, Weihong1,2,3,4,5
2020-05-01
发表期刊BIOCONJUGATE CHEMISTRY
ISSN1043-1802
通讯作者Wang, Ruowen(wangwrw@sjtu.edu.cn) ; Tan, Weihong(tan@hnu.edu.cn)
摘要Bispecific aptamer-drug conjugates (BsApDC) may improve the efficacy of drugs by enhancing cellular internalization and targeted delivery. Nevertheless, the synthesis of single-molecular BsApDC has not yet been reported, and it could be thwarted by synthetic challenges. Herein we report a general approach to synthesize a BsApDC hybridized chemical and biological method. Primers incorporated with 5-Fluorouracil (5-FU), 10-Hydroxycamptothecin, and Maleimidocaproyl-valinecitrulline-p-aminobenzoyloxycarbonyl-monomethyl auristatin E(vcMMAE) were prepared by chemical synthesis, which were converted to corresponding ApDCs efficiently by enzymatic reaction. Biological studies revealed that BsApDC binds with target cells with enhanced internalization and better inhibitory activity, demonstrating the potential of BsApDCs for targeted tumor therapy.
DOI10.1021/acs.bioconjchem.0c00071
关键词[WOS]NEXT-GENERATION ; DNA ; DELIVERY ; GROWTH ; CELLS
收录类别SCI
语种英语
资助项目NSFC[NSFC 21877079] ; NSFC[NSFC 81803068] ; ZJNSF[LY16B020001] ; NIH[GM R35 127130] ; NSF[1645215]
项目资助者NSFC ; ZJNSF ; NIH ; NSF
WOS研究方向Biochemistry & Molecular Biology ; Chemistry
WOS类目Biochemical Research Methods ; Biochemistry & Molecular Biology ; Chemistry, Multidisciplinary ; Chemistry, Organic
WOS记录号WOS:000537398400008
出版者AMER CHEMICAL SOC
引用统计
被引频次:14[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.hfcas.ac.cn:8080/handle/334002/103106
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, Renji Hosp, Inst Mol Med, Sch Med,State Key Lab Oncogenes & Related Genes, Shanghai 200240, Peoples R China
2.Shanghai Jiao Tong Univ, Coll Chem & Chem Engn, Shanghai 200240, Peoples R China
3.Hunan Univ, Coll Biol, State Key Lab Chemo Biosensing & Chemometr, Coll Chem & Chem Engn,Mol Sci & Biomed Lab MBL, Changsha 410082, Hunan, Peoples R China
4.Hunan Univ, Aptamer Engn Ctr Hunan Prov, Changsha 410082, Hunan, Peoples R China
5.Univ Chinese Acad Sci, Chinese Acad Sci, Canc Hosp, Inst Canc & Basic Med IBMC, Hangzhou 310022, Zhejiang, Peoples R China
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GB/T 7714
Sun, Yang,Gao, Fei,Yang, Cai,et al. Construction of Bispecific Aptamer-Drug Conjugate by a Hybrid Chemical and Biological Approach[J]. BIOCONJUGATE CHEMISTRY,2020,31.
APA Sun, Yang.,Gao, Fei.,Yang, Cai.,Li, Yingying.,Jin, Cheng.,...&Tan, Weihong.(2020).Construction of Bispecific Aptamer-Drug Conjugate by a Hybrid Chemical and Biological Approach.BIOCONJUGATE CHEMISTRY,31.
MLA Sun, Yang,et al."Construction of Bispecific Aptamer-Drug Conjugate by a Hybrid Chemical and Biological Approach".BIOCONJUGATE CHEMISTRY 31(2020).
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