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4-Anilino-6-phenyl-quinoline inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK2)

✍ Scribed by Henric Olsson; Peter Sjö; Oguz Ersoy; Anna Kristoffersson; Joakim Larsson; Bo Nordén

Publisher
Elsevier Science
Year
2010
Tongue
English
Weight
406 KB
Volume
20
Category
Article
ISSN
0960-894X

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✦ Synopsis

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-microM IC(50) values, and suppresses LPS-induced TNFalpha levels in THP-1 cells. MK2 inhibition kinetic measurements indicated mixed binding approaching non-ATP competitive inhibition.

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