Discovery and Development of Keap1-Nrf2 Protein-Protein Interaction Inhibitors

2018 ◽  
pp. 249-286
Author(s):  
Zhengyu Jiang ◽  
Qidong You
Keyword(s):  
Protein Interaction ◽  
Protein Protein Interaction ◽  
Nrf2 Protein

scholarly journals Emerging Screening Approaches in the Development of Nrf2–Keap1 Protein–Protein Interaction Inhibitors

2019 ◽  
Vol 20 (18) ◽  
pp. 4445 ◽  
Author(s):  
Chung-Hang Leung ◽  
Jia-Tong Zhang ◽  
Guan-Jun Yang ◽  
Hao Liu ◽  
Quan-Bin Han ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Protein Interaction ◽  
Developmental Process ◽  
Protein Protein Interaction ◽  
Lead Compounds ◽  
Disease Therapy ◽  
Molecular Databases ◽  
Viable Approach ◽  
Nrf2 Protein ◽  
Screening Approaches

Due to role of the Keap1–Nrf2 protein–protein interaction (PPI) in protecting cells from oxidative stress, the development of small molecule inhibitors that inhibit this interaction has arisen as a viable approach to combat maladies caused by oxidative stress, such as cancers, neurodegenerative disease and diabetes. To obtain specific and genuine Keap1–Nrf2 inhibitors, many efforts have been made towards developing new screening approaches. However, there is no inhibitor for this target entering the clinic for the treatment of human diseases. New strategies to identify novel bioactive compounds from large molecular databases and accelerate the developmental process of the clinical application of Keap1–Nrf2 protein–protein interaction inhibitors are greatly needed. In this review, we have summarized virtual screening and other methods for discovering new lead compounds against the Keap1–Nrf2 protein–protein interaction. We also discuss the advantages and limitations of different strategies, and the potential of this PPI as a drug target in disease therapy.

Fragment-growing guided design of Keap1-Nrf2 protein-protein interaction inhibitors for targeting myocarditis

2018 ◽  
Vol 117 ◽  
pp. 228-237 ◽  
Author(s):  
Ning Meng ◽  
Hua Tang ◽  
Hao Zhang ◽  
Chengshi Jiang ◽  
Li Su ◽  
...  
Keyword(s):  
Protein Interaction ◽  
Protein Protein Interaction ◽  
Nrf2 Protein

scholarly journals Modified Peptide Inhibitors of the Keap1–Nrf2 Protein–Protein Interaction Incorporating Unnatural Amino Acids

ChemBioChem ◽  
2018 ◽  
Vol 19 (17) ◽  
pp. 1810-1816 ◽  
Author(s):  
Nikolaos D. Georgakopoulos ◽  
Sandeep K. Talapatra ◽  
Jemma Gatliff ◽  
Frank Kozielski ◽  
Geoff Wells
Keyword(s):  
Amino Acids ◽  
Protein Interaction ◽  
Unnatural Amino Acids ◽  
Peptide Inhibitors ◽  
Protein Protein Interaction ◽  
Nrf2 Protein
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