一种新型的丝裂原激活蛋白激酶激活的蛋白激酶 2（MK2）抑制剂：4-苯胺基-6-苯基喹啉。
4-Anilino-6-phenyl-quinoline inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK2).
机构信息
Department of Biological Sciences, AstraZeneca R&D Lund, S-22187 Lund, Sweden.
出版信息
Bioorg Med Chem Lett. 2010 Aug 15;20(16):4738-40. doi: 10.1016/j.bmcl.2010.06.107. Epub 2010 Jun 25.
PMID:20643547
Abstract
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.
摘要
通过高通量筛选发现了一组丝裂原活化蛋白激酶激活的激酶 2（MK2）抑制剂。该化合物对酶具有亚微摩尔 IC50 值的活性，并抑制 LPS 诱导的 THP-1 细胞中 TNFalpha 的水平。MK2 抑制动力学测量表明，混合结合接近非 ATP 竞争性抑制。
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