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Review

Targeting Hypoxia and Angiogenesis through HIF-1? Inhibition

Juan A. Diaz-Gonzalez MD, James Russell, Ana Rouzaut, Ignacio Gil-Bazo and Luis Montuenga

volume 4 | issue 10

October 2005
Pages: 1055-1062

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Hypoxia is an important phenomenon in the tumor microenvironment. Hypoxic tumors are more aggressive and resistant to anti-neoplastic treatments. HIF-1? plays a major role in the response of tumors to hypoxia, and it is mainly responsible for the “angiogenic switch”. HIF-1? contributes to tumor aggressiveness, invasiveness, and resistance to radiotherapy and chemotherapy. Targeting HIF-1? is an attractive strategy, with the potential for disrupting multiple pathways crucial for tumor growth.. We review recent findings on the potential efficacy of small molecules to down-regulate HIF-1?. These promising drugs inhibit HIF-1? synthesis or transcriptional activity by blocking a variety of steps in several different signaling pathways. Blocking HIF-1? activity should not only down-regulate tumor angiogenesis, but also interfere with glycolytic metabolism and tumor cell growth. This strategy could also improve the efficiency of established tumor therapies.




We now provide open access to journal articles published online for one year or more. This article may be downloaded at the following link:

 Download PDF

If the document does not open, please right-click on the link (control-click on a Macintosh) and select the option to save the file to disk.