Structure-based lead identification of ATP-competitive MK2 inhibitors

Autor:	Judith Versteegh, Nicole Seegers, Henri Klop, Tjeerd Barf, Claudia Hofstra, Jeroen A.D.M. de Roos, Carsten Schultz-Fademrecht, Mario van Zeeland, Arthur Oubrie, Bert Kazemier, Maaike van Hoek, Dennis Demont, Allard Kaptein, Jorrit J. Hornberg, Sander de Wilde, Ruben L. Smeets, Bas van de Kar, Ruud van der Heijden, Richard van Someren
Rok vydání:	2011
Předmět:	Drug Models Molecular media_common.quotation_subject Clinical Biochemistry Pharmaceutical Science Computational biology Protein Serine-Threonine Kinases Crystallography X-Ray Auto-immunity transplantation and immunotherapy [N4i 4] Biochemistry Binding Competitive Inhibitory Concentration 50 Structure-Activity Relationship Adenosine Triphosphate In vivo Drug Discovery Animals Humans Molecular Biology Protein Kinase Inhibitors ADME media_common chemistry.chemical_classification biology Molecular Structure Drug discovery Kinase MAPKAPK2 Organic Chemistry Intracellular Signaling Peptides and Proteins Rats Disease Models Animal Enzyme chemistry Enzyme inhibitor Drug Design biology.protein Molecular Medicine Caco-2 Cells
Zdroj:	Bioorganic & Medicinal Chemistry Letters, 21, 3818-22 Bioorganic & Medicinal Chemistry Letters, 21, 12, pp. 3818-22
ISSN:	0960-894X
Popis:	Item does not contain fulltext MK2 kinase is a promising drug discovery target for the treatment of inflammatory diseases. Here, we describe the discovery of novel MK2 inhibitors using X-ray crystallography and structure-based drug design. The lead has in vivo efficacy in a short-term preclinical model.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1bdeec28829a3848ff7f20ab076a3584 http://hdl.handle.net/2066/97376 Zobrazit plný text záznamu Full Text from ScienceDirect