Journal
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
Volume 20, Issue 18, Pages -Publisher
MDPI
DOI: 10.3390/ijms20184445
Keywords
Keap1-Nrf2; protein-protein interaction; inhibitors; oxidative stress; virtual screening
Funding
- Hong Kong Baptist University [FRG2/17-18/003]
- Health and Medical Research Fund [HMRF/14150561]
- National Natural Science Foundation of China (China) [201575121, 21775131]
- Hong Kong Baptist University (China)
- Interdisciplinary Research Matching Scheme (China) [RC-IRMS/16-17/03]
- Interdisciplinary Research Clusters Matching Scheme (China) [RC-IRCs/17-18/03]
- Collaborative Research Fund (China) [C5026-16G]
- SKLEBA
- HKBU (China) [SKLP_1718_P04]
- Science and Technology Development Fund, Macau SAR [0072/2018/A2, SKL-QRCM-2017-2019]
- University of Macau (China) [MYRG2018-00187-ICMS]
Ask authors/readers for more resources
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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