| Literature DB >> 10956206 |
S W Djuric1, N Y BaMaung, A Basha, H Liu, J R Luly, D J Madar, R J Sciotti, N P Tu, F L Wagenaar, P E Wiedeman, X Zhou, S Ballaron, J Bauch, Y W Chen, X G Chiou, T Fey, D Gauvin, E Gubbins, G C Hsieh, K C Marsh, K W Mollison, M Pong, T K Shaughnessy, M P Sheets, M Smith, J M Trevillyan, U Warrior, C D Wegner, G W Carter.
Abstract
A series of bis(trifluoromethyl)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.Entities:
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Year: 2000 PMID： 10956206 DOI： 10.1021/jm990615a
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446