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Identification of 2,4‐Dinitro‐Biphenyl‐Based Compounds as MAPEG Inhibitors

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We identified 2,4-dinitro-biphenyl-based compounds as new inhibitors of leukotriene C4 synthase (LTC4S) and 5lipoxygenase-activating protein (FLAP), both members of the “membrane associated proteins in eicosanoid and glutathione metabolism” (MAPEG) family involved in the biosynthesis of proinflammatory eicosanoids. By molecular docking we evaluated the putative binding against the targets of interest, and by applying cellfree and cell-based assays we demon-strate inhibition of LTC4S and FLAP by the small molecules at low micromolar concentrations. The present results integrate the previously observed inhibitory profile of the tested compounds against another MAPEG member, i.e., microsomal pros-taglandin E2 synthase (mPGES)-1, suggesting that the 2,4-dinitro-biphenyl scaffold is a suitable molecular platform for a multitargeting approach to modulate pro-inflammatory mediators in inflammation and cancer treatment.

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