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Macrophage Migration Inhibitory Factor Acts as the Potential Target of a Newly Synthesized Compound, 1-(9'-methyl-3'-carbazole)-3, 4-dihydro-β-carboline.

Sci Rep. 2019-02; 
KoPin-Hao,ShenYa-Ching,MuruganKaliyappan,HuangChiung-Wei,SivakumarGovindan,PalPinki,LiaoChia-Ching,LuoKai-Shin,ChuangEric Y,TsaiMong-Hsun,LaiLiang-C
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Recombinant Proteins The hydrogen-deuterium exchange (HDX) of MIF recombinant human protein (GenScript, NJ, USA) was measured in the presence and absence of MCDC. Get A Quote

摘要

For a newly synthesized compound, identifying its target protein is a slow but pivotal step toward understand its pharmacologic mechanism. In this study, we systemically synthesized novel manzamine derivatives and chose 1-(9'-methyl-3'-carbazole)-3, 4-dihydro-β-carboline (MCDC) as an example to identify its target protein and function. MCDC had potent toxicity against several cancer cells. To identify its target protein, we first used a docking screen to predict macrophage migration inhibitory factor (MIF) as the potential target. Biochemical experiments, including mutation analysis and hydrogen-deuterium exchange assays, validated the binding of MCDC to MIF. Furthermore, MCDC was shown by microa... More

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