Discovery and Development of Kelch-like ECH-Associated Protein 1. Nuclear Factor Erythroid 2‑Related Factor 2 (KEAP1:NRF2) Protein–Protein Interaction Inhibitors: Achievements, Challenges, and Future Directions

• Published in: Journal of medicinal chemistry Vol. 59; no. 24; pp. 10837 - 10858
• Main Authors: Jiang, Zheng-Yu, Lu, Meng-Chen, You, Qi-Dong
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 22.12.2016
• Subjects: Animals; Drug Discovery; Humans; Kelch-Like ECH-Associated Protein 1 - antagonists & inhibitors; NF-E2-Related Factor 2 - antagonists & inhibitors; Protein Binding - drug effects; Small Molecule Libraries - chemistry; Small Molecule Libraries - pharmacology

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...