Novel MK2 Inhibitors by Fragment Screening
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
Keywords: MAPKAP kinase; MK2; TNFα; TROSY; fragment; p38α
Document Type: Research Article
Affiliations: Evotec AG,Schnackenburgallee 114, D-22525 Hamburg, Germany.
Publication date: August 1, 2009
- Combinatorial Chemistry & High Throughput Screening publishes full length original research articles and reviews describing various topics in combinatorial chemistry (e.g. small molecules, peptide, nucleic acid or phage display libraries) and/or high throughput screening (e.g. developmental, practical or theoretical). Ancillary subjects of key importance, such as robotics and informatics, will also be covered by the journal. In these respective subject areas, Combinatorial Chemistry & High Throughput Screening is intended to function as the most comprehensive and up-to-date medium available. The journal should be of value to individuals engaged in the process of drug discoveryand development, in the settings of industry, academia or government.
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