Abstract:
: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.
journal_name
Chem Biol Drug Desjournal_title
Chemical biology & drug designauthors
Kilty I,Green MP,Bell AS,Brown DG,Dodd PG,Hewson C,Hughes SJ,Phillips C,Ryckmans T,Smith RT,van Hoorn WP,Cohen P,Jones LHdoi
10.1111/cbdd.12169subject
Has Abstractpub_date
2013-11-01 00:00:00pages
500-5issue
5eissn
1747-0277issn
1747-0285journal_volume
82pub_type
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