丝裂原活化蛋白激酶激活的蛋白激酶2（MK-2）的氨基氰基吡啶抑制剂。
Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).
作者信息
Anderson David R, Hegde Shridhar, Reinhard Emily, Gomez Leslie, Vernier William F, Lee Len, Liu Shuang, Sambandam Aruna, Snider Patricia A, Masih Liaqat
机构信息
Pfizer Global Research and Development, 700 Chesterfield Parkway W, Chesterfield, MO 63017, USA.
出版信息
Bioorg Med Chem Lett. 2005 Mar 15;15(6):1587-90. doi: 10.1016/j.bmcl.2005.01.067.
A class of inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2) was discovered. These compounds have demonstrated activity against the enzyme with IC50 values as low as 130 nM and suppress the expression of TNFalpha in U937 cells. These represent the first small molecule inhibitors of MK-2 to be reported.
发现了一类有丝分裂原活化蛋白激酶激活的蛋白激酶2（MK-2）抑制剂。这些化合物已证明对该酶具有活性，IC50值低至130 nM，并能抑制U937细胞中TNFα的表达。这些是首次报道的MK-2小分子抑制剂。
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