Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2)

…, L Resnick, JE Sabalski, J Butera, J Liu, K Parris…

文献索引：Lovering, Frank; Kirincich, Steve; Wang, Weiheng; Combs, Kerry; Resnick, Lynn; Sabalski, Joan E.; Butera, John; Liu, Julie; Parris, Kevin; Telliez Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 9 p. 3342 - 3351

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被引用次数: 20

摘要

A novel series of inhibitors for mitogen activated protein kinase-activated protein kinase 2 (MK-2) are reported. These squarate based inhibitors were identified via a high-throughput screen. An MK2 co-structure with the starting ligand was obtained and a structure based approach was followed to optimize potency and selectivity.