A clinical drug library screen identifies clobetasol propionate as an NRF2 inhibitor with potential therapeutic efficacy in KEAP1 mutant lung cancer

The Kelch-like ECH-associated protein 1 (KEAP1)–nuclear factor E2-related factor 2 (NRF2)pathway has a central role in cellular antioxidant defense. NRF2 activation due to KEAP1 or NRF2 mutations occurs frequently in many cancers, suggesting that NRF2 inhibition could be a promising therapeutic stra...

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Veröffentlicht in:	Oncogene 2017-09, Vol.36 (37), p.5285-5295
Hauptverfasser:	Choi, E-J, Jung, B-J, Lee, S-H, Yoo, H-S, Shin, E-A, Ko, H-J, Chang, S, Kim, S-Y, Jeon, S-M
Format:	Artikel
Sprache:	eng
Schlagworte:	38/70 42/89 631/67/1059/602 631/67/1612/1350 631/67/2327 96/95 96/98 Animals Anti-Inflammatory Agents - pharmacology Antioxidants Apoptosis Cell Biology Cell Line, Tumor Clobetasol Clobetasol - pharmacology Development and progression Drug Screening Assays, Antitumor Drug therapy Genetic aspects Glucocorticoids Glycogen Glycogen synthase kinase 3 Health aspects Human Genetics Humans Internal Medicine Kelch-Like ECH-Associated Protein 1 - genetics Kinases LKB1 protein Lung cancer Lung Neoplasms - drug therapy Lung Neoplasms - genetics Lung Neoplasms - pathology Medicine Medicine & Public Health Mice, Inbred BALB C Mice, Nude Mutation NF-E2-Related Factor 2 - antagonists & inhibitors Oncology original-article Oxidative stress Patient outcomes Propionic acid Proteins Random Allocation Rapamycin Signal Transduction Transcription factors Tumors Xenograft Model Antitumor Assays
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