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Abstract
The transcription factor Nrf2 regulates the expression of a large network of cytoprotective and metabolic enzymes and proteins. Compounds that directly and reversibly inhibit the interaction between Nrf2 and its main negative regulator Keap1 are potential pharmacological agents for a range of disease types including neurodegenerative conditions and cancer. We describe the development of a series of 1,4-diphenyl-1,2,3-triazole compounds that inhibit the Nrf2-Keap1 protein-protein interaction (PPI) in vitro and in live cells and up-regulate the expression of Nrf2-dependent gene products.
Original language | English |
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Pages (from-to) | 7186-7194 |
Number of pages | 9 |
Journal | Journal of Medicinal Chemistry |
Volume | 58 |
Issue number | 18 |
DOIs | |
Publication status | Published - 24 Sept 2015 |
Keywords
- Cell Line, Tumor
- Click chemistry
- Computer simulation
- Databases, Chemical
- Dose-response relationship, Drug
- Fluorescence polarization
- HEK293 cells
- Heme oxygenase-1
- Humans
- Intracellular signaling Peptides and Proteins
- Isothiocyanates
- Molecular docking simulation
- NAD(P)H dehydrogenase (Quinone)
- NF-E2-related factor 2
- Protein binding
- Structure-activity relationship
- Triazoles
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery
- Medicine(all)
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