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Emerging Screening Approaches in the Development of Nrf2-Keap1 Protein-Protein Interaction Inhibitors
Leung, CH1; Zhang, JT1; Yang, GJ1; Liu, H2; Han, QB3; Ma, DL2
2019-09
Source PublicationINTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
ISSN1422-0067
Volume20Issue:18
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.

KeywordVirtual Screening Keap1-nrf2 Protein-protein Interaction Inhibitors Oxidative Stress
DOI10.3390/ijms20184445
Indexed BySCIE
Language英語English
WOS Research AreaBiochemistry & Molecular Biology ; Chemistry
WOS SubjectBiochemistry & Molecular Biology ; Chemistry, Multidisciplinary
WOS IDWOS:000489100500124
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Cited Times [WOS]:16   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Corresponding AuthorLeung, CH; Ma, DL
Affiliation1.University of Macau, Inst Chinese Med Sci, State Key Lab Qual Res Chinese Med, Macau 999078, Peoples R China
2.Hong Kong Baptist Univ, Dept Chem, Kowloon Tong, Hong Kong 999077, Peoples R China
3.Hong Kong Baptist Univ, Coll Int Educ, Sch Continuing Educ, Shek Mun, Hong Kong 999077, Peoples R China
First Author AffilicationUniversity of Macau
Corresponding Author AffilicationUniversity of Macau
Recommended Citation
GB/T 7714
Leung, CH,Zhang, JT,Yang, GJ,et al. Emerging Screening Approaches in the Development of Nrf2-Keap1 Protein-Protein Interaction Inhibitors[J]. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES,2019,20(18).
APA Leung, CH,Zhang, JT,Yang, GJ,Liu, H,Han, QB,&Ma, DL.(2019).Emerging Screening Approaches in the Development of Nrf2-Keap1 Protein-Protein Interaction Inhibitors.INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES,20(18).
MLA Leung, CH,et al."Emerging Screening Approaches in the Development of Nrf2-Keap1 Protein-Protein Interaction Inhibitors".INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES 20.18(2019).
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