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

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

Volume: 18 Issue: 4

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

Affiliation:

• Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009,China

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

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.

Cite this article as:

Wei Jinlian, Yang Yingrui, Lu Mengchen, Lei Yonghua, Xu Lili, Jiang Zhengyu, Xu Xiaoli, Guo Xiaoke, Zhang Xiaojin, Sun Haopeng*, You Qidong, Recent Advances in the Discovery of HIF-1α-p300/CBP Inhibitors as Anti-Cancer Agents, Mini-Reviews in Medicinal Chemistry 2018; 18 (4) . https://dx.doi.org/10.2174/1389557516666160630124938