In vitro benchmarking of NF-κB inhibitors

NF-κB 抑制剂的体外基准测试

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作者:Alexandria P Harrold, Megan M Cleary, Narendra Bharathy, Melvin Lathara, Noah E Berlow, Nicholas K Foreman, Andrew M Donson, Vladimir Amani, William J Zuercher, Charles Keller

Abstract

Dysregulated activity of the transcription factors of the nuclear factor κb (NF-κB) family has been implicated in numerous cancer types, inflammatory diseases, autoimmune disease, and other disorders. As such, selective NF-κB pathway inhibition is an attractive target to researchers for preclinical and clinical drug development. A plethora of commercially and clinically available inhibitors claim to be NF-κB specific; however, such claims of specificity are rarely quantitative or benchmarked, making the biomedical literature difficult to contextualize. This imprecision is worsened because some NF-κB reporter systems have low signal-to-noise ratios. Herein, we use a robust, defined, commercially available reporter system to benchmark NF-κB agonists and antagonists for the field. We also functionally characterize a RELA fusion-positive ependymoma cell culture with validated NF-κB inhibitor compounds.

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