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Quantitative conformational profiling of kinase inhibitors reveals origins of selectivity for Aurora kinase activation states

Protein kinases undergo large-scale structural changes that tightly regulate function and control recognition by small-molecule inhibitors. Methods for quantifying the conformational effects of inhibitors and linking them to an understanding of selectivity patterns have long been elusive. We have de...

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Detalles Bibliográficos
Autores principales: Lake, Eric W., Muretta, Joseph M., Thompson, Andrew R., Rasmussen, Damien M., Majumdar, Abir, Faber, Erik B., Ruff, Emily F., Thomas, David D., Levinson, Nicholas M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: National Academy of Sciences 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6304972/
https://www.ncbi.nlm.nih.gov/pubmed/30518564
http://dx.doi.org/10.1073/pnas.1811158115