- 3,5-Bis(trifluoromethyl)pyrazoles: A novel class of NFAT transcription factor regulator
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A series of bis(trifiuoromethyl)pyrazoles (BTPs) has been found to be a novel inhibitor of cytokine production. Identified initially as inhibitors of IL-2 synthesis, the BTPs have been optimized in this regard and even inhibit IL-2 production with a 10-fold enhancement over cyclosporine in an ex vivo assay. Additionally, the BTPs show inhibition of IL-4, IL-5, IL-8, and eotaxin production. Unlike the IL-2 inhibitors, cyclosporine and FK506, the BTPs do not directly inhibit the dephosphorylation of NFAT by calcineurin.
- Djuric,Wiedeman,Zhou,Ballaron,Bauch,Chen,Chiou,Fey,Gauvin,Gubbins,Hsieh,Bamaung,Marsh,Mollison,Pong,Shaughnessy,Sheets,Smith,Trevillyan,Warrior,Wegner,Carter,Basha,Liu,Luly,Madar,Sciotti,Tu,Wagenaar
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p. 2975 - 2981
(2007/10/03)
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