Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2)

[Display omitted] 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 IC 50 values as low as 130 nM and suppress the expression of TNFα in U937 cells. These represent the first...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2005-03, Vol.15 (6), p.1587-1590
Main Authors: Anderson, David R., Hegde, Shridhar, Reinhard, Emily, Gomez, Leslie, Vernier, William F., Lee, Len, Liu, Shuang, Sambandam, Aruna, Snider, Patricia A., Masih, Liaqat
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Gene Expression
Humans
Kinase inhibitor
MAP Kinase Kinase 2 - antagonists & inhibitors
Medical sciences
MK-2
Models, Chemical
Molecular Structure
Pharmacology. Drug treatments
Pyridines - chemistry
Pyridines - pharmacology
Rats
Structure-Activity Relationship
TNFα
Tumor Necrosis Factor-alpha - metabolism
U937 Cells
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Summary:[Display omitted] 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 IC 50 values as low as 130 nM and suppress the expression of TNFα in U937 cells. These represent the first small molecule inhibitors of MK-2 to be reported.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.01.067