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Site-specific construction of triptolide-based antibody-drug conjugates
2021-12-01
发表期刊BIOORGANIC & MEDICINAL CHEMISTRY (IF:3.3[JCR-2023],3.1[5-Year])
ISSN0968-0896
EISSN1464-3391
卷号51
DOI10.1016/j.bmc.2021.116497
摘要Antibody-drug conjugates (ADCs) have emerging as efficient agents to target deliver cytotoxic drugs and reduce their off-target side effects. Triptolide has attracted attention to be used in ADC development. Herein, three rationally designed triptolide drug-linkers have been synthesized for use in site-specific construction of ADCs. Carbamates that were supposed to be more stable than carbonates were introduced to attach triptolide to the linkers. PEG and discrete PEG chains were incorporated to improve the hydrophilicity of drug-linkers. The ADCs were finally site-specifically prepared by conjugation of the drug-linkers to trastuzumab through disulfide rebridging approach. The preliminary anti-tumor activities of these ADCs were evaluated and they displayed high potencies against HER2-targeted cancer in vitro and in vivo.
关键词Antibody-drug conjugates Triptolide Site-specific construction
收录类别SCIE ; IC
语种英语
WOS研究方向Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
WOS类目Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
WOS记录号WOS:000722146000002
出版者PERGAMON-ELSEVIER SCIENCE LTD
原始文献类型Article
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文献类型期刊论文
条目标识符https://kms.shanghaitech.edu.cn/handle/2MSLDSTB/133136
专题物质科学与技术学院_博士生
免疫化学研究所_特聘教授组_抗体化学实验室
免疫化学研究所_公共科研平台_分析化学平台
生命科学与技术学院_硕士生
通讯作者Li, Jiusheng; Jiang, Biao; Chen, Hongli
作者单位
1.Chinese Acad Sci, Shanghai Adv Res Inst, Shanghai 201210, Peoples R China;
2.ShanghaItech Univ, Shanghai Inst Adv Immunochem Studies, 393 Middle Huaxia Rd, Shanghai 201210, Peoples R China;
3.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
第一作者单位免疫化学研究所
通讯作者单位免疫化学研究所
推荐引用方式
GB/T 7714
Wei, Ding,Mao, Yurong,Xu, Zili,et al. Site-specific construction of triptolide-based antibody-drug conjugates[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2021,51.
APA Wei, Ding.,Mao, Yurong.,Xu, Zili.,Chen, Jiakang.,Li, Jiusheng.,...&Chen, Hongli.(2021).Site-specific construction of triptolide-based antibody-drug conjugates.BIOORGANIC & MEDICINAL CHEMISTRY,51.
MLA Wei, Ding,et al."Site-specific construction of triptolide-based antibody-drug conjugates".BIOORGANIC & MEDICINAL CHEMISTRY 51(2021).
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