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
Hauptverfasser: Olsson, Henric, Sjö, Peter, Ersoy, Oguz, Kristoffersson, Anna, Larsson, Joakim, Nordén, Bo
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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.06.107