IMR Press / FBL / Volume 12 / Issue 9 / DOI: 10.2741/2329

Frontiers in Bioscience-Landmark (FBL) is published by IMR Press from Volume 26 Issue 5 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on as a courtesy and upon agreement with Frontiers in Bioscience.

Open Access Article
Targeting tumors with hypoxia-activated cytotoxins
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1 Division of Radiation and Cancer Biology, Department of Radiation Oncology, Stanford University School of Medicine, Stanford, CA94305-5152, U.S.A.
Academic Editors:Olga Greco, Simon Scott
Front. Biosci. (Landmark Ed) 2007, 12(9), 3483–3501;
Published: 1 May 2007
(This article belongs to the Special Issue The tumor microenvironment as a target for therapy)

This review focuses on the recent development of hypoxia-activated cytotoxins. Such drugs are prodrugs activated to cytotoxic products in the hypoxic environment of solid tumors (so-called "bioreductive prodrugs"), but can also be activated by radiation (radiation-activated prodrugs). These compounds grew out of research on hypoxic radiosensitizers, which are compounds that can overcome the radiation resistance of hypoxic cells, and we will discuss this area also. The advantages and limitations of each class of the hypoxia-activated cytotoxins are discussed. In addition we will discuss a novel method of targeting drugs to tumors based on anaerobic bacteria, the so-called "clostridia-directed enzyme prodrug therapy" or CDEPT, which also exploits the hypoxic environment of solid tumors.

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