Multifunctional Tumor-Targeting Cathepsin B-Sensitive Gemcitabine Prodrug Covalently Targets Albumin in Situ and Improves Cancer Therapy

被引：20

作者：

Zhang, Huicong ^{[1
]}

Su, Zhisu ^{[1
]}

Wang, Kuanglei ^{[2
,3
]}

Li, Na ^{[4
]}

Chen, Hongxiang ^{[5
]}

Tan, Xiao ^{[6
]}

Li, Lingxiao ^{[7
,8
]}

He, Zhonggui ^{[1
]}

Sun, Jin ^{[1
]}

机构：

[1] Shenyang Pharmaceut Univ, Wuya Coll Innovat, Dept Pharmaceut, 59 Mailbox,103 Wenhua Rd, Shenyang 110016, Liaoning, Peoples R China

[2] Wuyi Univ, Jiangmen 529020, Guangdong, Peoples R China

[3] Int Healthcare Innovat Inst Jiangmen, Jiangmen 529080, Guangdong, Peoples R China

[4] Shenyang Pharmaceut Univ, Wuya Coll Innovat, Clin Pharm, Shenyang 110016, Liaoning, Peoples R China

[5] China Food & Drug Adm, Ctr Drug Evaluat, Beijing 100022, Peoples R China

[6] Shenyang Pharmaceut Univ, Sch Pharm, Shenyang 110016, Liaoning, Peoples R China

[7] Queens Univ Belfast, Sch Pharm, 97 Lisburn Rd, Belfast BT9 7BL, Antrim, North Ireland

[8] China Med Univ, Sch Pharm, Shenyang 110013, Liaoning, Peoples R China

来源：

BIOCONJUGATE CHEMISTRY | 2018年 / 29卷 / 06期

基金：

中国国家自然科学基金;

关键词：

RESISTANCE; DELIVERY;

D O I：

10.1021/acs.bioconjchem.8b00223

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

We report a new type of amide bond-bearing cathepsin B-sensitive gemcitabine (GEM) prodrugs, capable of in situ covalently targeting circulating albumin and then making a hitchhike to the tumor. Specially, less plasma-enzyme deactivation, long plasma half-life, independence on nucleoside transporters, outstanding tumor targeting, and site-specific drug release are achieved, and as such these multifunctional advantages contribute to the dramatically increased in vivo antitumor efficacy.

引用

页码：1852 / 1858

页数：7

共 20 条

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