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

Binding thermodynamics and kinetics guided optimization of potent Keap1–Nrf2 peptide inhibitors

RSC Advances ◽  
2015 ◽  
Vol 5 (105) ◽  
pp. 85983-85987 ◽  
Author(s):  
Meng-Chen Lu ◽  
Zhi-Yun Chen ◽  
Ya-Lou Wang ◽  
Yong-Lin Jiang ◽  
Zhen-Wei Yuan ◽  
...  
Keyword(s):  
Protein Interaction ◽  
Peptide Inhibitors ◽  
Research Interest ◽  
Novel Agents ◽  
Binding Thermodynamics ◽  
Protein Protein Interaction ◽  
Thermodynamics And Kinetics ◽  
Nrf2 Protein

Activation of Nrf2 by directly inhibiting the Keap1–Nrf2 Protein–Protein Interaction (PPI) has gained research interest with regard to developing novel agents for treating inflammatory related diseases.

Optimization of linear and cyclic peptide inhibitors of KEAP1-NRF2 protein-protein interaction

2020 ◽  
Vol 28 (21) ◽  
pp. 115738
Author(s):  
Stefania Colarusso ◽  
Daniele De Simone ◽  
Tommaso Frattarelli ◽  
Matteo Andreini ◽  
Mauro Cerretani ◽  
...  
Keyword(s):  
Protein Interaction ◽  
Cyclic Peptide ◽  
Peptide Inhibitors ◽  
Protein Protein Interaction ◽  
Nrf2 Protein

Peptide inhibitors of the Keap1–Nrf2 protein–protein interaction

2012 ◽  
Vol 52 (2) ◽  
pp. 444-451 ◽  
Author(s):  
Rowena Hancock ◽  
Hélène C. Bertrand ◽  
Tadayuki Tsujita ◽  
Shama Naz ◽  
Ayman El-Bakry ◽  
...  
Keyword(s):  
Protein Interaction ◽  
Peptide Inhibitors ◽  
Protein Protein Interaction ◽  
Nrf2 Protein

Peptide inhibitors of the Keap1–Nrf2 protein–protein interaction with improved binding and cellular activity

2013 ◽  
Vol 11 (21) ◽  
pp. 3553 ◽  
Author(s):  
Rowena Hancock ◽  
Marjolein Schaap ◽  
Helene Pfister ◽  
Geoff Wells
Keyword(s):  
Protein Interaction ◽  
Peptide Inhibitors ◽  
Cellular Activity ◽  
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.

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