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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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Bibliografiske detaljer
Udgivet i:Nat Chem Biol
Main Authors: Chaikuad, Apirat, Tacconi, Eliana, Zimmer, Jutta, Liang, Yanke, Gray, Nathanael S., Tarsounas, Madalena, Knapp, Stefan
Format: Artigo
Sprog:Inglês
Udgivet: 2014
Fag:
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4687050/
https://ncbi.nlm.nih.gov/pubmed/25195011
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/nchembio.1629
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