Recent Advances in the Discovery of HIF-1α-p300/CBP Inhibitors as Anti-Cancer Agents

Author(s): Jinlian Wei, Yingrui Yang, Mengchen Lu, Yonghua Lei, Lili Xu, Zhengyu Jiang, Xiaoli Xu, Xiaoke Guo, Xiaojin Zhang, Haopeng Sun*, Qidong You

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 18 , Issue 4 , 2018

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Graphical Abstract:


Hypoxia-inducible factor-1 (HIF-1), a heterodimeric (containing α and β subunits) transcription factor, is involved in hypoxia response pathway that regulates the expression of many tumorrelated genes. The stabilized HIF-1 heterodimer couples to the general co-activators p300/CBP (CREB binding protein), forming an active transcription factor to initiate hypoxic responses. Inhibiting the transcription factor-coactivator HIF-1α-p300/CBP interaction represents an attractive approach for blocking hypoxia pathway in tumors. Recently, diverse HIF-1α-p300/CBP inhibitors have been designed and their anti-tumor activities have been evaluated. The developments of inhibitors of HIF-1α- p300/CBP are discussed in this review. An outline of structures and biological activities of these inhibitors can be traced, along with the approaches for inhibitors discovery. The challenges in identifying novel and selective potent inhibitors of HIF-1α-p300/CBP are also put forward.

Keywords: Anticancer, cancer therapy, HIF-1α/p300 inhibitors, hypoxia response pathway, hypoxia-inducible factor-1, p300/CREB binding protein.

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Article Details

Year: 2018
Page: [296 - 309]
Pages: 14
DOI: 10.2174/1389557516666160630124938
Price: $65

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