Emerging Screening Approaches in the Development of Nrf2-Keap1 Protein-Protein Interaction Inhibitors
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.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2019 |
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| Erschienen: |
2019 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:20 |
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| Enthalten in: |
International journal of molecular sciences - 20(2019), 18 vom: 10. Sept. |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Leung, Chung-Hang [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 10.02.2020 Date Revised 10.02.2020 published: Electronic Citation Status MEDLINE |
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| doi: |
10.3390/ijms20184445 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM301185832 |
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| 500 | |a published: Electronic | ||
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| 520 | |a 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 | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Review | |
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| 650 | 4 | |a inhibitors | |
| 650 | 4 | |a oxidative stress | |
| 650 | 4 | |a protein–protein interaction | |
| 650 | 4 | |a virtual screening | |
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| 650 | 7 | |a Kelch-Like ECH-Associated Protein 1 |2 NLM | |
| 650 | 7 | |a NF-E2-Related Factor 2 |2 NLM | |
| 650 | 7 | |a NFE2L2 protein, human |2 NLM | |
| 650 | 7 | |a Small Molecule Libraries |2 NLM | |
| 700 | 1 | |a Zhang, Jia-Tong |e verfasserin |4 aut | |
| 700 | 1 | |a Yang, Guan-Jun |e verfasserin |4 aut | |
| 700 | 1 | |a Liu, Hao |e verfasserin |4 aut | |
| 700 | 1 | |a Han, Quan-Bin |e verfasserin |4 aut | |
| 700 | 1 | |a Ma, Dik-Lung |e verfasserin |4 aut | |
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