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Eur J Med Chem. 2012 Mar;49:24-40. doi: 10.1016/j.ejmech.2012.01.033. Epub 2012 Jan 24.

Recent advances in hypoxia-inducible factor (HIF)-1 inhibitors.

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  • 1College of Pharmacy, Dongguk University-Seoul, Seoul, Republic of Korea.


Tumor hypoxia has been recognized as a common feature of solid tumors and a negative prognostic factor for response to treatment and survival of cancer patients. The discovery of hypoxia-inducible factor-1 (HIF-1), a molecular determinant of responses to hypoxia in mammalian cells, has renewed enthusiasm for discovery and development of targeted therapies exploiting the hypoxic tumor microenvironment. HIF-1 activity in tumors depends on availability of the HIF-1α subunit, the levels of which increase under hypoxic conditions and through activation of oncogenes and/or inactivation of tumor suppressor genes. Increased HIF-1 has been correlated with increased angiogenesis, aggressive tumor growth, and poor patient prognosis, leading to current interest in HIF-1 as promising anticancer drug target. In spite of an ever increasing number of putative small molecule inhibitors of HIF-1, only a few are progressing through preclinical and early clinical development. In this review, we will discuss recent advances in discovery and development of small molecule inhibitors that target the HIF-1 pathway as potential anticancer agents.

Copyright © 2012 Elsevier Masson SAS. All rights reserved.

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