scholarly journals Profiling Environmental Chemicals for Activity in the Antioxidant Response Element Signaling Pathway Using a High Throughput Screening Approach

2012 ◽  
Vol 120 (8) ◽  
pp. 1150-1156 ◽  
Author(s):  
Sunita J Shukla ◽  
Ruili Huang ◽  
Steven O Simmons ◽  
Raymond R Tice ◽  
Kristine L Witt ◽  
...  
Keyword(s):  
Signaling Pathway ◽  
High Throughput ◽  
High Throughput Screening ◽  
Antioxidant Response ◽  
Environmental Chemicals ◽  
Antioxidant Response Element ◽  
Response Element ◽  
Screening Approach

scholarly journals LAS0811: From Combinatorial Chemistry to Activation of Antioxidant Response Element

2009 ◽  
Vol 2009 ◽  
pp. 1-8 ◽  
Author(s):  
Ming Zhu ◽  
Hyounggee Baek ◽  
Ruiwu Liu ◽  
Aimin Song ◽  
Kit Lam ◽  
...  
Keyword(s):  
Small Molecules ◽  
Combinatorial Chemistry ◽  
High Throughput Screening ◽  
Cancer Chemoprevention ◽  
Antioxidant Response ◽  
Heme Oxygenase 1 ◽  
Related Factor ◽  
Antioxidant Response Element ◽  
Response Element ◽  
Enhanced Production

The antioxidant response element (ARE) and its transcription factor, nuclear factor-erythroid 2 p45-related factor 2 (Nrf2), are potential targets for cancer chemoprevention. We sought to screen small molecules synthesized with combinatorial chemistry for activation of ARE. By high-throughput screening of 9400 small molecules from 10 combinatorial chemical libraries using HepG2 cells with an ARE-driven reporter, we have identified a novel small molecule, 1,2-dimethoxy-4,5-dinitrobenzene (LAS0811), as an activator of the ARE. LAS0811 upregulated the activity of NAD(P)H:quinone oxidoreductase 1 (NQO1), a representative antioxidative enzyme regulated by ARE. It enhanced production of an endogenous reducing agent, glutathione (GSH). In addition, LAS0811 induced expression of heme oxygenase 1 (HO1), which is an ARE-regulated enzyme with anti-inflammatory activity. Furthermore, LAS0811 reduced cell death due to the cytotoxic stress of a strong oxidant, t-butyl hydroperoxide (t-BOOH). Mechanistically, LAS0811 upregulated the expression of Nrf2 and promoted its translocation into the nuclei leading to subsequent ARE activation. Taken together, LAS0811 is a novel activator of the ARE and its associated detoxifying genes and, thus, a potential agent for cancer chemoprevention.

scholarly journals Corrigendum: The Nrf2-Antioxidant Response Element Signaling Pathway Controls Fibrosis and Autoimmunity in Scleroderma

2021 ◽  
Vol 12 ◽  
Author(s):  
Niloufar Kavian ◽  
Souad Mehlal ◽  
Mohamed Jeljeli ◽  
Nathaniel Edward Bennett Saidu ◽  
Carole Nicco ◽  
...  
Keyword(s):  
Signaling Pathway ◽  
Antioxidant Response ◽  
Antioxidant Response Element ◽  
Response Element

scholarly journals The Nrf2-Antioxidant Response Element Signaling Pathway Controls Fibrosis and Autoimmunity in Scleroderma

2018 ◽  
Vol 9 ◽  
Author(s):  
Niloufar Kavian ◽  
Souad Mehlal ◽  
Mohamed Jeljeli ◽  
Nathaniel Edward Bennett Saidu ◽  
Carole Nicco ◽  
...  
Keyword(s):  
Signaling Pathway ◽  
Antioxidant Response ◽  
Antioxidant Response Element ◽  
Response Element

scholarly journals Assessment of the DNA damaging potential of environmental chemicals using a quantitative high-throughput screening approach to measure p53 activation

2017 ◽  
Vol 58 (7) ◽  
pp. 494-507 ◽  
Author(s):  
Kristine L. Witt ◽  
Jui-Hua Hsieh ◽  
Stephanie L. Smith-Roe ◽  
Menghang Xia ◽  
Ruili Huang ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Environmental Chemicals ◽  
Screening Approach ◽  
P53 Activation
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