Cargando…
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...
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: | |
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 |
Ejemplares similares
-
Comparative structural analyses and nucleotide-binding characterization of the four KH domains of FUBP1
por: Ni, Xiaomin, et al.
Publicado: (2020) -
Interplay between Fanconi anemia and homologous recombination pathways in genome integrity
por: Michl, Johanna, et al.
Publicado: (2016) -
Assessing reversible and irreversible binding effects of kinase covalent inhibitors through ADP-Glo assays
por: Schröder, Martin, et al.
Publicado: (2021) -
Mutation in the Common Docking Domain Affects MAP Kinase ERK2 Catalysis and Stability
por: Novak, Leonore, et al.
Publicado: (2023) -
Targeting the Alternative
Vitamin E Metabolite Binding
Site Enables Noncanonical PPARγ Modulation
por: Arifi, Silvia, et al.
Publicado: (2023)