- Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).
Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).
Bioorganic & medicinal chemistry (2009-04-15)
Frank Lovering, Steve Kirincich, Weiheng Wang, Kerry Combs, Lynn Resnick, Joan E Sabalski, John Butera, Julie Liu, Kevin Parris, J B Telliez
PMID19364658
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.
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