Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973)

[Image: see text] The ERK/MAP kinase cascade is a key mechanism subject to dysregulation in cancer and is constitutively activated or highly upregulated in many tumor types. Mutations associated with upstream pathway components RAS and Raf occur frequently and contribute to the oncogenic phenotype t...

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Detalhes bibliográficos
Main Authors: Rice, Kenneth D., Aay, Naing, Anand, Neel K., Blazey, Charles M., Bowles, Owen J., Bussenius, Joerg, Costanzo, Simona, Curtis, Jeffry K., Defina, Steven C., Dubenko, Larisa, Engst, Stefan, Joshi, Anagha A., Kennedy, Abigail R., Kim, Angie I., Koltun, Elena S., Lougheed, Julie C., Manalo, Jean-Claire L., Martini, Jean-Francois, Nuss, John M., Peto, Csaba J., Tsang, Tsze H., Yu, Peiwen, Johnston, Stuart
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2012
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4025802/
https://ncbi.nlm.nih.gov/pubmed/24900486
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml300049d
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