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Molecules 2017, 22(6), 883; doi:10.3390/molecules22060883

Identification of Non-Electrophilic Nrf2 Activators from Approved Drugs

1
Hubei Key Laboratory of Agricultural Bioinformatics, College of Informatics, Huazhong Agricultural University, Wuhan 430070, China
2
Shanghai Thinkgene Biotech Co., LTD., Shanghai 200000, China
The first two authors contributed equally.
*
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 5 May 2017 / Revised: 22 May 2017 / Accepted: 24 May 2017 / Published: 26 May 2017
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Abstract

Oxidative damage can lead to a wide range of diseases. Nrf2 is an important transcription factor that regulates many of the cytoprotective enzymes involved in the oxidative stress response. Therefore, targeting the regulation of Nrf2 activation is one logical and effective strategy to prevent or lower the risk of oxidative stress-related diseases. Until now, most research has focused on electrophilic indirect Nrf2 activators, but the risk of ‘off-target’ effects may be associated with these activators. To find novel small non-electrophilic modulators of Nrf2, we started from chemical agents derived from a connectivity map (cMap) and identified 22 non-electrophilic potential Nrf2-activating drugs through a drug repositioning tactic. By determining the expression changes of antioxidant genes in MCF7 cells that were treated with the potential Nrf2 activators using quantitative real-time polymerase chain reaction RT-PCR (real-time polymerase chain reaction) (qRT-PCR), astemizole was found to have a greater scale of upregulating antioxidant genes NQO1, HO-1, and GCLM than the positive control d,l-sulforaphane, although the testing concentration was lower than that of the control. Astemizole is a good potential redox regulator and deserves more pharmacodynamic experimentation to test and verify its feasibility for use as an Nrf2 activator. View Full-Text
Keywords: oxidative stress; Nrf2 activator; drug repositioning; redox regulators oxidative stress; Nrf2 activator; drug repositioning; redox regulators
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Zhang, Q.-Y.; Chu, X.-Y.; Jiang, L.-H.; Liu, M.-Y.; Mei, Z.-L.; Zhang, H.-Y. Identification of Non-Electrophilic Nrf2 Activators from Approved Drugs. Molecules 2017, 22, 883.

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