TAK1 inhibition in the DFG-out conformation
- Kilty, Iain
- Green, Martin P.
- Bell, Andrew S.
- Brown, David G.
- Dodd, Peter G.
- Hewson, Christopher
- Hughes, Samantha J.
- Phillips, Christopher
- Ryckmans, Thomas
- Smith, Robert T.
- van Hoorn, Willem P.
- Cohen, Philip
- Jones, Lyn H.
Publication date
November 2013
DOIAbstract
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. 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.</p
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