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Your search keyword '"Huppertz, Christine"' showing total 3 results
Start Over Author "Huppertz, Christine" Topic tumor necrosis factors
3 results on '"Huppertz, Christine"'

2. Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy

Author

Velcicky, Juraj, Feifel, Roland, Hawtin, Stuart, Heng, Richard, Huppertz, Christine, Koch, Guido, Kroemer, Markus, Moebitz, Henrik, Revesz, Laszlo, Scheufler, Clemens, and Schlapbach, Achim

Subjects
*PYRAZOLES, *PHOSPHORYLATION, *ENZYME inhibitors, *TUMOR necrosis factors, *CHEMICAL reactions, *ANTINEOPLASTIC agents
Abstract

Abstract: New, selective 3-aminopyrazole based MK2-inhibitors were discovered by scaffold hopping strategy. The new derivatives proved to inhibit intracellular phosphorylation of hsp27 as well as LPS-induced TNFα release in cells. In addition, selected derivative 14e also inhibited LPS-induced TNFα release in vivo. [Copyright &y& Elsevier]

Published
2010
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3. Pyrrolo-pyrimidones: A novel class of MK2 inhibitors with potent cellular activity

Author

Schlapbach, Achim, Feifel, Roland, Hawtin, Stuart, Heng, Richard, Koch, Guido, Moebitz, Henrik, Revesz, Laszlo, Scheufler, Clemens, Velcicky, Juraj, Waelchli, Rudolf, and Huppertz, Christine

Subjects
*ENZYME inhibitors, *RHEUMATOID arthritis, *PHOSPHORYLATION, *HEAT shock proteins, *TUMOR necrosis factors
Abstract

Abstract: Pyrrolo-pyrimidones of the general structure 1 were synthesized and evaluated for their potential as MK2 inhibitors. Potent derivatives were discovered which inhibit MK2 in the nanomolar range and show potent inhibition of cytokine release from LPS-stimulated monocytes. These derivatives were shown to inhibit phosphorylation of hsp27, a downstream target of MK2 and are modestly selective in a panel of 28 kinases. [Copyright &y& Elsevier]

Published
2008
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