TAK1 inhibition in the DFG-out conformation.

Autor: Kilty I; Pfizer World Wide Research and Development, Ramsgate Road, Sandwich, CT13 9NJ, UK; BioTherapeutics Research and Development, Pfizer, Cambridge, MA, 02140, USA., Green MP, Bell AS, Brown DG, Dodd PG, Hewson C, Hughes SJ, Phillips C, Ryckmans T, Smith RT, van Hoorn WP, Cohen P, Jones LH
Jazyk: angličtina
Zdroj: Chemical biology & drug design [Chem Biol Drug Des] 2013 Nov; Vol. 82 (5), pp. 500-5.
DOI: 10.1111/cbdd.12169
Abstrakt: The first example of an inhibitor of the kinase TAK1 that binds in the DFG-out conformation is disclosed. These preliminary studies used kinase-targeted screening and structure-based drug design to create a molecule with dual pharmacological inhibition of p38 and TAK1 that demonstrated significant activity in a cell-based, anti-inflammatory assay.
(© 2013 John Wiley & Sons A/S.)
Databáze: MEDLINE
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