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Enzymatic activation of indolequinone-substituted 5-fluorodeoxyuridine prodrugs in hypoxic cells.

Author: JihoYota, KawaiKiyohiko, KuriharaRyohsuke, TanabeKazuhito, UtoYoshihiro, YamadaHisatsugu

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Overview

IQ-FdUrd, a 5-fluorodeoxyuridine (FdUrd) prodrug bearing an indolequinone unit, is a substrate of reductases and is activated to release FdUrd under hypoxic conditions. This study characterized the enzymatic reaction of IQ-FdUrd and confirmed its selective cytotoxicity in hypoxic tumor cells.
Paper Details　
Original Abstract of the Article :
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...See full text at original site
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引用元：
https://doi.org/10.1016/j.bmcl.2019.04.003

データ提供：米国国立医学図書館（NLM）

Hypoxia-Targeted Drug Delivery: A New Approach for Cancer Treatment

Solid tumors often exhibit hypoxic conditions, a characteristic that poses a challenge for effective drug delivery. This research investigates a novel approach for hypoxia-targeted drug delivery using 5-fluorodeoxyuridine (FdUrd) prodrugs bearing an indolequinone unit (IQ-FdUrd). The study examines the enzymatic activation of these prodrugs under hypoxic conditions, potentially offering a targeted strategy for cancer therapy.

Delivering the Goods: Targeting Hypoxic Tumor Cells with IQ-FdUrd

The study demonstrates that IQ-FdUrd prodrugs can be selectively activated under hypoxic conditions, releasing FdUrd, a potent anticancer agent, specifically in hypoxic tumor cells. This finding highlights the potential of IQ-FdUrd as a hypoxia-targeted drug delivery system, potentially offering a more effective and targeted approach to cancer treatment. Imagine IQ-FdUrd as a clever camel caravan that navigates the treacherous landscape of hypoxic tumor cells, strategically delivering the payload of FdUrd, directly attacking the cancer cells.

Precision Medicine: A New Era in Cancer Treatment

The study's findings underscore the importance of developing targeted drug delivery systems for cancer treatment. By harnessing the unique characteristics of hypoxic tumor cells, IQ-FdUrd could pave the way for a new era of precision medicine, potentially leading to more effective and less toxic therapies for cancer patients.

Dr.Camel's Conclusion

This research explores the potential of IQ-FdUrd as a hypoxia-targeted drug delivery system, offering a novel strategy for treating cancer. It's like a caravan of camels carrying a precious cargo of FdUrd, carefully navigating through the treacherous desert landscape of hypoxic tumors, delivering the therapeutic payload directly to the target. This study presents a promising new approach for fighting cancer, showcasing the power of precision medicine.

Date :
  1. Date Completed 2020-09-11
  2. Date Revised 2020-09-11
Further Info :

Pubmed ID

30975626

DOI: Digital Object Identifier

10.1016/j.bmcl.2019.04.003

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English

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