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

  作者 Olsson, H; Sjo, P; Ersoy, O; Kristoffersson, A; Larsson, J; Norden, B  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2010年20-16;  页码  4738-4740  
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[摘要]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-mu M IC50 values, and suppresses LPS-induced TNF alpha levels in THP-1 cells. MK2 inhibition kinetic measurements indicated mixed binding approaching non-ATP competitive inhibition. (C) 2010 Elsevier Ltd. All rights reserved.

 
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