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Bioorg Med Chem Lett ; 15(6): 1587-90, 2005 Mar 15.
Article in English | MEDLINE | ID: mdl-15745802

ABSTRACT

A class of inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2) was discovered. These compounds have demonstrated activity against the enzyme with IC50 values as low as 130 nM and suppress the expression of TNFalpha in U937 cells. These represent the first small molecule inhibitors of MK-2 to be reported.


Subject(s)
MAP Kinase Kinase 2/antagonists & inhibitors , Pyridines/chemistry , Pyridines/pharmacology , Animals , Gene Expression , Humans , Models, Chemical , Molecular Structure , Rats , Structure-Activity Relationship , Tumor Necrosis Factor-alpha/metabolism , U937 Cells
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