2012Journal of Gastroenterology and HepatologyOpen access

Hypoxia‐inducible factor‐1 as a therapeutic target in cancer

Ceen‐Ming Tang, Jun Yu

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Abstract

Hypoxia-inducible factor-1 (HIF-1) is a transcription factor that immortalizes tumors by inducing key genes in cancer biology, including angiogenesis, glycolysis, invasion, and metastasis. Overexpression of HIF-1α is thus associated with resistance to cancer chemotherapy and increased patient mortality in several cancer phenotypes. In the present review, we summarize the role of intratumoral hypoxia and bioactive lipids in enhancing HIF-1 activity, critically discussing the potential for HIF-1α inhibitors in cancer chemotherapy. Considering preclinical studies, HIF-1 inhibitors appear to have antitumor effects and thus represent a novel therapeutic strategy.

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Hypoxia-inducible factor-1 (HIF-1) is a transcription factor that immortalizes tumors by inducing key genes in cancer biology, including angiogenesis, glycolysis, invasion, and metastasis. Overexpression of HIF-1α is thus associated with resistance to cancer chemotherapy and increased patient mortality in several cancer phenotypes. In the present review, we summarize the role of intratumoral hypoxia and bioactive lipids in enhancing HIF-1 activity, critically discussing the potential for HIF-1α inhibitors in cancer chemotherapy. Considering preclinical studies, HIF-1 inhibitors appear to have antitumor effects and thus represent a novel therapeutic strategy.

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Available abstract

Hypoxia-inducible factor-1 (HIF-1) is a transcription factor that immortalizes tumors by inducing key genes in cancer biology, including angiogenesis, glycolysis, invasion, and metastasis. Overexpression of HIF-1α is thus associated with resistance to cancer chemotherapy and increased patient mortality in several cancer phenotypes. In the present review, we summarize the role of intratumoral hypoxia and bioactive lipids in enhancing HIF-1 activity, critically discussing the potential for HIF-1α inhibitors in cancer chemotherapy. Considering preclinical studies, HIF-1 inhibitors appear to have antitumor effects and thus represent a novel therapeutic strategy.

Key concepts: Medicine, Hypoxia (environmental), Angiogenesis, Metastasis, Transcription factor, Hypoxia-Inducible Factor 1, HIF1A, Cancer research

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