Author(s): Oliver Keminer, Joachim Kraemer, Jan Kahmann, Ina Sternberger, Christoph Scheich, Joern Jungmann, Sabine Schaertl, Dirk Winkler, Osamu Ichihara, Mark Whittaker, Dirk Ullmann and Thomas Hesterkamp
Page: [697 - 703] Pages: 7
* (Excluding Mailing and Handling)
Inhibitors of MAPKAP kinase 2 (MK2) are expected to attenuate the p38α signal transduction pathway in macrophages in a similar way to p38α 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, TNFα-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
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