Protease-Activated Drug Development

被引：187
作者：
Choi, Ki Young [1 ]
Swierczewska, Magdalena [1 ,2 ]
Lee, Seulki [1 ]
Chen, Xiaoyuan [1 ]
机构：
[1] NIBIB, LOMIN, NIH, Bethesda, MD 20892 USA
[2] SUNY Stony Brook, Dept Biomed Engn, Stony Brook, NY 11794 USA
来源：
THERANOSTICS | 2012年 / 2卷 / 02期
基金：
美国国家卫生研究院;
关键词：
Protease; activatable probe; Alzheimer's disease; cancer; caspase; cathepsin; kallikrein; MMP; PSA; serine protease; aspartyl protease; PROSTATE-SPECIFIC ANTIGEN; ALBUMIN-BINDING PRODRUG; L-LEUCYL-DOXORUBICIN; SENSITIVE PHOTODYNAMIC AGENTS; COPOLYMER-BOUND ADRIAMYCIN; SQUAMOUS-CELL CARCINOMAS; TRANSGENIC MOUSE MODEL; BREAST-CANCER PATIENTS; HUMAN CATHEPSIN-B; MATRIX METALLOPROTEINASES;
D O I：
10.7150/thno.4068
中图分类号：
R-3 [医学研究方法]; R3 [基础医学];
学科分类号：
1001 ;
摘要：
In this extensive review, we elucidate the importance of proteases and their role in drug development in various diseases with an emphasis on cancer. First, key proteases are introduced along with their function in disease progression. Next, we link these proteases as targets for the development of prodrugs and provide clinical examples of protease-activatable prodrugs. Finally, we provide significant design considerations needed for the development of the next generation protease-targeted and protease-activatable prodrugs.
引用
收藏
页码：156 / 178
页数：23
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