| Autor: |
Djuric, S. W., BaMaung, N. Y., Basha, A., Liu, H., Luly, J. R., Madar, D. J., Sciotti, R. J., Tu, N. P., Wagenaar, F. L., Wiedeman, P. E., Zhou, X., Ballaron, S., Bauch, J., Chen, Y.-W., Chiou, X. G., Fey, T., Gauvin, D., Gubbins, E., Hsieh, G. C., Marsh, K. C., Mollison, K. W., Pong, M., Shaughnessy, T. K., Sheets, M. P., Smith, M., Trevillyan, J. M., Warrior, U., Wegner, C. D., Carter, G. W. |
| Zdroj: |
Journal of Medicinal Chemistry; August 10, 2000, Vol. 43 Issue: 16 p2975-2981, 7p |
| Abstrakt: |
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. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
|
