4.7 Article

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

期刊

BIOCONJUGATE CHEMISTRY
卷 29, 期 6, 页码 1852-1858

出版社

AMER CHEMICAL SOC
DOI: 10.1021/acs.bioconjchem.8b00223

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  1. National Natural Science Foundation of China [81473164, 81573371, 81773656]

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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.

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