Journal of Medicinal Chemistry p. 7186 - 7194 (2015)
Update date:2022-08-02
Topics:
Bertrand, Hélène C.
Schaap, Marjolein
Baird, Liam
Georgakopoulos, Nikolaos D.
Fowkes, Adrian
Thiollier, Clarisse
Kachi, Hiroko
Dinkova-Kostova, Albena T.
Wells, Geoff
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.
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