KEAP1型
转录因子
化学
调节器
计算生物学
小分子
鉴定(生物学)
蛋白质-蛋白质相互作用
生物
生物化学
基因
植物
作者
Zhengyu Jiang,Meng-Chen Lu,Qidong You
标识
DOI:10.1021/acs.jmedchem.6b00586
摘要
The transcription factor Nrf2 is the primary regulator of the cellular defense system, and enhancing Nrf2 activity has potential usages in various diseases, especially chronic age-related and inflammatory diseases. Recently, directly targeting Keap1-Nrf2 protein-protein interaction (PPI) has been an emerging strategy to selectively and effectively activate Nrf2. This Perspective summarizes the progress in the discovery and development of Keap1-Nrf2 PPI inhibitors, including the Keap1-Nrf2 regulatory mechanisms, biochemical techniques for inhibitor identification, and approaches for identifying peptide and small-molecule inhibitors, as well as discusses privileged structures and future directions for further development of Keap1-Nrf2 PPI inhibitors.
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