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ShanghaiTech University Knowledge Management System
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]) |
ISSN | 0968-0896 |
EISSN | 1464-3391 |
卷号 | 51 |
DOI | 10.1016/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 |
引用统计 | 正在获取...
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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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