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Long-circulating enzyme-activated HSP90-targeted camptothecin derivatives

文献类型：期刊论文

作者Ding, Mengyuan1,3,4; Shen, Qianqian1,2; Su, Yi1,2; Lu, Yingxin3; Jin, Jiyu3; Chen, Yi2; Lu, Wei3; Fang, Yanfen1,2; Zhu, Shulei4
刊名JOURNAL OF CONTROLLED RELEASE
出版日期2025-07-10
卷号383页码:16
关键词eHSP90 Camptothecin derivatives Cathepsin B Long-circulating
ISSN号0168-3659
DOI10.1016/j.jconrel.2025.113839
英文摘要Drug delivery technology has emerged as an effective strategy to enhance the anti-tumor potential of camptothecins. In this study, we constructed an enzyme-activated targeted drug release system employing a stable valine-alanine linker in combination with a highly cytotoxic camptothecin derivative, AZ ' 0132. The prodrug, named HC07, was successfully delivered to the tumor site via eHSP90, where it underwent specific cleavage, thereby enhancing its therapeutic window and reducing ocular toxicity. In order to further improve its metabolic properties, we innovatively combined HC07 with plasma endogenous albumin to construct albumin-binding prodrugs HC08 and HC09 for the first time. These prodrugs demonstrated prolonged circulation times in vivo and significantly improved tumor selectivity and anti-tumor efficacy. This work presents a promising eHSP90based long-circulating drug delivery system, providing new avenues for the design of future anti-cancer drugs.
WOS关键词MOLECULAR CHAPERONES ; EXTRACELLULAR HSP90 ; DRUG-DELIVERY ; INHIBITORS ; CONJUGATE
资助项目Science and Technology Commission of Shanghai Municipality[21140902000] ; Shanghai Rising-Star Program[24QB2700300]
WOS研究方向Chemistry ; Pharmacology & Pharmacy
语种英语
WOS记录号WOS:001494932600003
出版者ELSEVIER
源URL[http://119.78.100.183/handle/2S10ELR8/317977]  
专题新药研究国家重点实验室
通讯作者Lu, Wei; Fang, Yanfen; Zhu, Shulei
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China
3.East China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug Dev, Sch Chem & Mol Engn, 3663 North Zhongshan Rd, Shanghai 200062, Peoples R China
4.East China Normal Univ, Innovat Ctr AI & Drug Discovery, Sch Pharm, 3663 North Zhongshan Rd, Shanghai 200062, Peoples R China
推荐引用方式
GB/T 7714		 Ding, Mengyuan,Shen, Qianqian,Su, Yi,et al. Long-circulating enzyme-activated HSP90-targeted camptothecin derivatives[J]. JOURNAL OF CONTROLLED RELEASE,2025,383:16.
APA Ding, Mengyuan.,Shen, Qianqian.,Su, Yi.,Lu, Yingxin.,Jin, Jiyu.,...&Zhu, Shulei.(2025).Long-circulating enzyme-activated HSP90-targeted camptothecin derivatives.JOURNAL OF CONTROLLED RELEASE,383,16.
MLA Ding, Mengyuan,et al."Long-circulating enzyme-activated HSP90-targeted camptothecin derivatives".JOURNAL OF CONTROLLED RELEASE 383(2025):16.

入库方式： OAI收割

来源：上海药物研究所

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