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Small molecules targeting HIF-1α pathway for cancer therapy in recent years
1Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan 250012, PR China.
Abstract:
Hypoxia is a very important feature of tumors, especially for solid tumors, and it was demonstrated highly relevant with aggressive biology, including anti-apoptosis, vasculogenesis and radiation or chemotherapy resistance. Correlatively, hypoxia-inducible factors 1-α (HIF-1α), which the wildest contribution of hypoxia-inducible factors (HIFs), plays a crucial role in the adaptation of tumor cells to hypoxia via upregulating the transcription of the oncogene and downregulating the transcription of suppressor gene. This review focus on the HIF-1α regulation including hydroxylation and acetylation, growth factors pathway, heat shock proteins(HSPs), and small molecule inhibitors for HIF-1α directly or indirectly.
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