Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series

[Image: see text] To increase kinase selectivity in an aminopyrazole-based PAK1 inhibitor series, analogues were designed to interact with the PAK1 deep-front pocket pre-DFG residue Thr-406, a residue that is hydrophobic in most kinases. This goal was achieved by installing lactam head groups to the...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Rudolph, Joachim, Aliagas, Ignacio, Crawford, James J., Mathieu, Simon, Lee, Wendy, Chao, Qi, Dong, Ping, Rouge, Lionel, Wang, Weiru, Heise, Christopher, Murray, Lesley J., La, Hank, Liu, Yanzhou, Manning, Gerard, Diederich, François, Hoeflich, Klaus P.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2015
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4468403/
https://ncbi.nlm.nih.gov/pubmed/26101579
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00151
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