A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics

Activation of the ERK pathway is a hallmark of cancer and targeting of upstream signalling partners led to the development of approved drugs. Recently SCH772984 has been shown to be a selective and potent ERK1/2 inhibitor. Here we report the structural mechanism for its remarkable selectivity. In ER...

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Detalles Bibliográficos
Autores principales: Chaikuad, Apirat, Tacconi, Eliana, Zimmer, Jutta, Liang, Yanke, Gray, Nathanael S., Tarsounas, Madalena, Knapp, Stefan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: 2014
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4687050/
https://www.ncbi.nlm.nih.gov/pubmed/25195011
http://dx.doi.org/10.1038/nchembio.1629

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4687050/
https://www.ncbi.nlm.nih.gov/pubmed/25195011
http://dx.doi.org/10.1038/nchembio.1629

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