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TAK 1 Inhibition in the DFG ‐Out Conformation
Author(s) -
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.,
Hoorn Willem P.,
Cohen Philip,
Jones Lyn H.
Publication year - 2013
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12169
Subject(s) - chemistry , kinase , protein kinase a , biochemistry
The first example of an inhibitor of the kinase TAK 1 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 TAK 1 that demonstrated significant activity in a cell‐based, anti‐inflammatory assay.