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Discovery of Bifunctional Oncogenic Target Inhibitors against Allosteric Mitogen-Activated Protein Kinase (MEK1) and Phosphatidylinositol 3-Kinase (PI3K)

The synthesis of a series of single entity, bifunctional MEK1/PI3K inhibitors achieved by covalent linking of structural analogs of the ATP-competitive PI3K inhibitor ZSTK474 and the ATP-noncompetitive MEK inhibitor PD0325901 is described. Inhibitors displayed potent in vitro inhibition of MEK1 (0.0...

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Bibliografische gegevens
Gepubliceerd in:J Med Chem
Hoofdauteurs: Van Dort, Marcian E., Hong, Hao, Wang, Hanxiao, Nino, Charles A., Lombardi, Rachel L., Blanks, Avery E., Galbán, Stefanie, Ross, Brian D.
Formaat: Artigo
Taal:Inglês
Gepubliceerd in: 2016
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Online toegang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4841451/
https://ncbi.nlm.nih.gov/pubmed/26943489
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.5b01655
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