Characterization of the Potent, Selective Nrf2 Activator, 3-(Pyridin-3-Ylsulfonyl)-5-(Trifluoromethyl)-2
| Autor: | John G, Yonchuk, Joseph P, Foley, Brian J, Bolognese, Gregory, Logan, William E, Wixted, Jen-Pyng, Kou, Diana G, Chalupowicz, Heidi G, Feldser, Yolanda, Sanchez, Hong, Nie, James F, Callahan, Jeffrey K, Kerns, Patricia L, Podolin |
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| Rok vydání: | 2017 |
| Předmět: |
NF-E2-Related Factor 2
Blotting Western Gene Expression Transfection Cell Line Pulmonary Disease Chronic Obstructive Ozone Coumarins Drug Discovery NAD(P)H Dehydrogenase (Quinone) Animals Humans Sulfones RNA Small Interfering Rats Wistar Lung Cell Nucleus Smoking Epithelial Cells Pneumonia Glutathione Mice Inbred C57BL Disease Models Animal Oxidative Stress Protein Transport HEK293 Cells |
| Zdroj: | The Journal of pharmacology and experimental therapeutics. 363(1) |
| ISSN: | 1521-0103 |
| Popis: | Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) is a key regulator of oxidative stress and cellular repair and can be activated through inhibition of its cytoplasmic repressor, Kelch-like ECH-associated protein 1 (Keap1). Several small molecule disrupters of the Nrf2-Keap1 complex have recently been tested and/or approved for human therapeutic use but lack either potency or selectivity. The main goal of our work was to develop a potent, selective activator of NRF2 as protection against oxidative stress. In human bronchial epithelial cells, our Nrf2 activator, 3-(pyridin-3-ylsulfonyl)-5-(trifluoromethyl)-2 |
| Databáze: | OpenAIRE |
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