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Mini Rev Med Chem. 2018;18(4):296-309. doi: 10.2174/1389557516666160630124938.

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

Wei J1,2, Yang Y1,2, Lu M1,2, Lei Y1,2, Xu L1,2, Jiang Z1,2, Xu X1,2, Guo X1,2, Zhang X1,2,3, Sun H1,2,4, You Q1,2.

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Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, P.R. China.
State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, P.R. China.
Department of Organic Chemistry, School of Science, China Pharmaceutical University, Nanjing 210009, P.R. China.
Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, P.R. China.


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.


Anticancer; HIF-1α/p300 inhibitors; cancer therapy; hypoxia response pathway; hypoxia-inducible factor-1; p300/CREB binding protein

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