Abstract：
: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.
journal_name
Int J Mol Scijournal_title
International journal of molecular sciencesauthors
Leung CH,Zhang JT,Yang GJ,Liu H,Han QB,Ma DLdoi
10.3390/ijms20184445subject
Has Abstractpub_date
2019-09-10 00:00:00issue
18issn
1422-0067pii
ijms20184445journal_volume
20pub_type
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