In vitro benchmarking of NF-κB inhibitors.
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ID: 91404
2020
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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.
| Reference Key |
harrold2020ineuropean
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| Authors | Harrold, Alexandria P;Cleary, Megan M;Bharathy, Narendra;Lathara, Melvin;Berlow, Noah E;Foreman, Nicholas K;Donson, Andrew M;Amani, Vladimir;Zuercher, William J;Keller, Charles; |
| Journal | European journal of pharmacology |
| Year | 2020 |
| DOI |
S0014-2999(20)30073-X
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