4-Anilino-6-phenyl-quinoline inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK2)
Compound 2g was found effective in reducing LPS-induced TNFα production in THP-1 cells, in a manner consistent with MK2 enzyme inhibition. A class of inhibitors of mitogen activated protein kinase-activated kinase 2 (MK2) was discovered via high-throughput screening. This compound class demonstrates...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2010-08, Vol.20 (16), p.4738-4740 |
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Hauptverfasser: | , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | Compound
2g was found effective in reducing LPS-induced TNFα production in THP-1 cells, in a manner consistent with MK2 enzyme inhibition.
A class of inhibitors of mitogen activated protein kinase-activated kinase 2 (MK2) was discovered via high-throughput screening. This compound class demonstrates activity against the enzyme with sub-μM IC
50 values, and suppresses LPS-induced TNFα levels in THP-1 cells. MK2 inhibition kinetic measurements indicated mixed binding approaching non-ATP competitive inhibition. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2010.06.107 |