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Cell Cycle. 2004 Feb;3(2):172-5.

Targeting topoisomerase I to inhibit hypoxia inducible factor 1.

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Developmental Therapeutics Program, Science Applications International Corporation, Frederick, Inc; National Cancer Institute at Frederick, Frederick, Maryland 21702, USA.


HIF-1 is a key factor in cancer progression. Efforts are underway to identify and develop small molecules that inhibit HIF-1 transcriptional activity. What are the best targets and the best ways to develop HIF-1 inhibitors are open questions. However, several "nonselective" HIF-1 inhibitors have been identified, which are either in the clinic or under development. In this article, we discuss how topoisomerase I poisons, which inhibit HIF-1a protein accumulation and transcriptional activity, can be "rationally" used to target HIF-1 for cancer therapy.

[Indexed for MEDLINE]

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