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Comb Chem High Throughput Screen. 2009 Aug;12(7):697-703. Epub 2009 Aug 1.

Novel MK2 inhibitors by fragment screening.

Author information

1
Evotec AG, Hamburg, Germany.

Abstract

Inhibitors of MAPKAP kinase 2 (MK2) are expected to attenuate the p38alpha signal transduction pathway in macrophages in a similar way to p38alpha inhibitors and to have a lower propensity for toxic side effects that have slowed the clinical development of the latter. Therefore, novel MK2 inhibitors may find therapeutic application in acute and chronic, TNFalpha-mediated inflammatory conditions like rheumatoid arthritis and others. Herein we have applied fragment screening, using physiologically relevant bioassays and fragment binding mode mapping by protein-observed NMR spectroscopy to the discovery of novel efficient chemical starting points for MK2.

PMID:
19531016
[Indexed for MEDLINE]

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