Abstract
The discovery of a series of potent, carboline-based MK2 inhibitors is described. These compounds inhibit MK2 with IC50s as low as 10 nM, as measured in a DELFIA assay. An X-ray crystal structure reveals that they bind in a region near the p-loop and the hinge region of MK2a.
MeSH terms
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology
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Carbolines / chemistry*
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Carbolines / pharmacology*
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Intracellular Signaling Peptides and Proteins / antagonists & inhibitors*
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Models, Molecular
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Molecular Structure
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Protein Serine-Threonine Kinases / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Carbolines
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Intracellular Signaling Peptides and Proteins
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MAP-kinase-activated kinase 2
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Protein Serine-Threonine Kinases