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Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction

A high-throughput screen (HTS) of the MLPCN library using a homogenous fluorescence polarization assay identified a small molecule as a first-in-class direct inhibitor of Keap1-Nrf2 protein-protein interaction. The HTS hit has three chiral centers; a combination of flash and chiral chromatographic s...

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Main Authors:	Hu, Longqin, Magesh, Sadagopan, Chen, Lin, Wang, Lili, Lewis, Timothy A., Chen, Yu, Khodier, Carol, Inoyama, Daigo, Beamer, Lesa J., Emge, Thomas J., Shen, Jian, Kerrigan, John E., Kong, Ah-Ng Tony, Dandapani, Sivaraman, Palmer, Michelle, Schreiber, Stuart L., Munoz, Benito
פורמט:	Artigo
שפה:	Inglês
יצא לאור:	2013
נושאים:	Article
גישה מקוונת:	https://ncbi.nlm.nih.gov/pmc/articles/PMC3648997/ https://ncbi.nlm.nih.gov/pubmed/23562243 https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2013.03.013
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Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction

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