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Structure-based lead identification of ATP-competitive MK2 inhibitors

Tjeerd Barf1, Allard Kaptein, Sander de Wilde

  • 1Merck Research Laboratories, MSD, Oss, The Netherlands.

Bioorganic & Medicinal Chemistry Letters
|May 14, 2011
PubMed

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.

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