Structure-Guided Design and Initial Studies of a Bifunctional MEK/PI3K Inhibitor (ST-168)

[Image: see text] The structure-based design of a new single entity, MEK/PI3K bifunctional inhibitor (7, ST-168), which displays improved MEK1 and PI3K isoform inhibition, is described. ST-168 demonstrated a 2.2-fold improvement in MEK1 inhibition and a 2.8-, 2.7-, 23-, and 2.5-fold improved inhibit...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Van Dort, Marcian E., Galbán, Stefanie, Nino, Charles A., Hong, Hao, Apfelbaum, April A., Luker, Gary D., Thurber, Greg M., Atangcho, Lydia, Besirli, Cagri G., Ross, Brian D.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2017
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5554897/
https://ncbi.nlm.nih.gov/pubmed/28835793
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.7b00111
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