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Structure-based lead identification of ATP-competitive MK2 inhibitors |
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| Authors: | Barf Tjeerd Kaptein Allard de Wilde Sander van der Heijden Ruud van Someren Richard Demont Dennis Schultz-Fademrecht Carsten Versteegh Judith van Zeeland Mario Seegers Nicole Kazemier Bert van de Kar Bas van Hoek Maaike de Roos Jeroen Klop Henri Smeets Ruben Hofstra Claudia Hornberg Jorrit Oubrie Arthur |
| Institution: | Merck Research Laboratories, MSD, PO Box 20, 5340 BH Oss, The Netherlands |
| Abstract: | 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. |
| Keywords: | MAPKAPK2 MK2 Anti-TNFα SBDD Rheumatoid arthritis |
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