期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 29, 期 11, 页码 1304-1307出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.04.003
关键词
Enzymatic activation; Prodrug; Tumor hypoxia; Reductase
资金
- Aoyama Gakuin University
- Ministry of Education, Culture, Sports, Science and Technology (MEXT), Japan [23113508]
Among the various enzymes, reductases that catalyze one-electron reduction are involved in the selective activation of functional compounds or materials in hypoxia, which is one of the well-known pathophysiological characteristics of solid tumors. Enzymatic one-electron reduction has been recognized as a useful reaction that can be applied in the design of tumor hypoxia-targeting drugs. In this report, we characterized the enzymatic reaction of 5-fluorodeoxyuridine (FdUrd) prodrug bearing an indolequinone unit (IQ-FdUrd), which is a substrate of reductases. IQ-FdUrd was activated to release FdUrd under hypoxic conditions after treatment with cytochrome NADPH P450 reductase. We also confirmed that IQ-FdUrd showed selective cytotoxicity in hypoxic tumor cells.
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