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

Autor:	John A. Butera, Weiheng Wang, Joan E. Sabalski, Julie Liu, Lynn Resnick, Kevin D. Parris, Jean-Baptiste Telliez, Kerry Combs, Frank Lovering, Steven J. Kirincich
Rok vydání:	2009
Předmět:	Models Molecular Clinical Biochemistry Pharmaceutical Science Biochemistry Monocytes Inhibitory Concentration 50 Structure-Activity Relationship Cell Line Tumor Drug Discovery Humans Transferase Protein kinase A Protein Kinase Inhibitors Molecular Biology Mitogen-Activated Protein Kinase 1 chemistry.chemical_classification Binding Sites biology Tumor Necrosis Factor-alpha Chemistry Organic Chemistry Ligand (biochemistry) In vitro Protein Transport Enzyme Enzyme inhibitor Drug Design Mitogen-activated protein kinase biology.protein Molecular Medicine Tumor necrosis factor alpha Cyclobutanes
Zdroj:	Bioorganic & Medicinal Chemistry. 17:3342-3351
ISSN:	0968-0896
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::90348df20fa278de0e487146df5bfba2 https://doi.org/10.1016/j.bmc.2009.03.041 Zobrazit plný text záznamu Full Text from ScienceDirect