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

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.

A novel series of inhibitors for mitogen activated protein kinase-activated protein kinase 2 (MK-2) are reported. An MK-2 co-structure was obtained and a structure based approach was followed to optimize potency and selectivity.Figure optionsDownload as PowerPoint slide