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Effects of Histone Deacetylase Inhibitors on HIF-1

Dongming Liang, Xianguo Kong and Nianli Sang

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Hypoxia inducible factors (HIF) are the master transcriptional regulators of angiogenesis and energy metabolism in mammals. Histone deacetylase inhibitors (HDAIs) are among the promising anti-cancer compounds currently in clinical trials. In addition to inducing hyperacetylation of histones, HDAIs have been found to repress HIF function, which has been construed as an important pharmacological mechanism underlying the HDAI-mediated repression of tumor growth and angiogenesis. While HDAIs are potent inhibitors of HIF function and thus may be useful in the prevention and treatment of cancers, a major dilemma is that they may induce hyperacetylation of non-specific targets thus causing side effects. A better understanding is now required of the molecular and biochemical mechanisms underlying the anti-HIF effects of these compounds. Here we summarize the recent advances towards a better understanding of these molecular and biochemical mechanisms.

Authors

Dongming Liang

Thomas Jefferson University, Philadelphia, PA

Xianguo Kong

Thomas Jefferson University, Philadelphia, PA

Nianli Sang

Thomas Jefferson University, Philadelphia, PA

This is an open-access article

 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.