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Design, synthesis of auristatins-glucuronide conjugates targeting the β-glucuronidase in tumor microenvironment

文献类型：期刊论文

作者Wang, Yujie3; Xu, Keshi2; Liu, Hongchun1; Zhang, Wei2; Hu, Chun2; Li, Yingxia3
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
出版日期2023-10-15
卷号95页码:5
关键词Auristatin E beta-Glucuronidase Antiproliferation Tumor microenvironment
ISSN号0960-894X
DOI10.1016/j.bmcl.2023.129493
通讯作者Hu, Chun(chunhu@syphu.edu.cn) ; Li, Yingxia(liyx417@fudan.edu.cn)
英文摘要Auristatins-glucuronide conjugates designed targeting the beta-Glucuronidase in tumor microenvironment were synthesized and evaluated on stabilities, the release of auristatins and the antitumor activities in this study. Conjugates 20 and 21 showed remarkable stabilities in phosphate buffer and bovine serum solution, and excellent selectivity between the in vitro antiproliferative activities against beta-glucuronidase pretreated and untreated cancer cells (IC50 = 5.7 nM similar to 9.7 nM, IC50 (-Enz) > 1 NM). Furthermore, conjugate 20 showed potent antitumor efficacy in HCT-116 xenograft mouse model without inducing side effects.
WOS关键词DOLASTATIN 10 ; DRUG ; ANTIBODY ; PRODRUG ; ACTIVATION
资助项目National Natural Science Foundation of China[U1906212] ; National Key R & D Program of China[2018YF0310905]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:001099883500001
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/307866]  
专题中国科学院上海药物研究所
通讯作者Hu, Chun; Li, Yingxia
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China
2.Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, Key Lab Struct based Drug Design & Discovery, Minist Educ China, Shenyang 110016, Peoples R China
3.Fudan Univ, Sch Pharm, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Wang, Yujie,Xu, Keshi,Liu, Hongchun,et al. Design, synthesis of auristatins-glucuronide conjugates targeting the β-glucuronidase in tumor microenvironment[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2023,95:5.
APA Wang, Yujie,Xu, Keshi,Liu, Hongchun,Zhang, Wei,Hu, Chun,&Li, Yingxia.(2023).Design, synthesis of auristatins-glucuronide conjugates targeting the β-glucuronidase in tumor microenvironment.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,95,5.
MLA Wang, Yujie,et al."Design, synthesis of auristatins-glucuronide conjugates targeting the β-glucuronidase in tumor microenvironment".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 95(2023):5.

入库方式： OAI收割

来源：上海药物研究所

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