Structure-based lead identification of ATP-competitive MK2 inhibitors.

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Title:	Structure-based lead identification of ATP-competitive MK2 inhibitors.
Author(s):	Barf, T.; Kaptein, A.; Wilde, S. de; Heijden, R. van der; Someren, R. van; Demont, D.; Schultz-Fademrecht, C.; Versteegh, J.; Zeeland, M. van; Seegers, N.; Kazemier, B.; Kar, B. van de; Hoek, M. van; Roos, J. de; Klop, H.; Smeets, R.L. ; Hofstra, C.; Hornberg, J.; Oubrie, A.
Publication year:	2011
Source:	Bioorganic & Medicinal Chemistry Letters, vol. 21, iss. 12, (2011), pp. 3818-3822
ISSN:	0960-894X
DOI:	https://doi.org/10.1016/j.bmcl.2011.04.018
Publication type:	Article / Letter to editor
Please use this identifier to cite or link to this item : https://hdl.handle.net/2066/97376
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Subject:	N4i 4: Auto-immunity, transplantation and immunotherapy
Organization:	Laboratory of Clinical Chemistry
Journal title:	Bioorganic & Medicinal Chemistry Letters
Volume:	vol. 21
Issue:	iss. 12
Page start:	p. 3818
Page end:	p. 3822
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.