Anderson David R, Meyers Marvin J, Kurumbail Ravi G, Caspers Nicole, Poda Gennadiy I, Long Scott A, Pierce Betsy S, Mahoney Matthew W, Mourey Robert J
Pfizer Global Research and Development, St Louis Laboratories, Chesterfield, MO 63017, USA.
Bioorg Med Chem Lett. 2009 Aug 15;19(16):4878-81. doi: 10.1016/j.bmcl.2009.02.015. Epub 2009 Feb 8.
Identification of potent benzothiophene inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK2), structure-activity relationship (SAR) studies, selectivity assessments against CDK2, cellular potency and mechanism of action are presented. Crystallographic data provide a rationale for the observed MK2 potency as well as selectivity over CDK2 for this class of inhibitors.
本文介绍了有丝分裂原活化蛋白激酶激活的蛋白激酶2（MK2）强效苯并噻吩抑制剂的鉴定、构效关系（SAR）研究、针对细胞周期蛋白依赖性激酶2（CDK2）的选择性评估、细胞活性及作用机制。晶体学数据为这类抑制剂所观察到的MK2活性以及对CDK2的选择性提供了理论依据。
