(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells

SET domain containing (lysine methyltransferase) 7 (SETD7) is implicated in multiple signaling and disease related pathways with a broad diversity of reported substrates. Here, we report the discovery of (R)-PFI-2—a first-in-class, potent (K(i)(app) = 0.33 nM), selective, and cell-active inhibitor o...

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Detalhes bibliográficos
Main Authors: Barsyte-Lovejoy, Dalia, Li, Fengling, Oudhoff, Menno J., Tatlock, John H., Dong, Aiping, Zeng, Hong, Wu, Hong, Freeman, Spencer A., Schapira, Matthieu, Senisterra, Guillermo A., Kuznetsova, Ekaterina, Marcellus, Richard, Allali-Hassani, Abdellah, Kennedy, Steven, Lambert, Jean-Philippe, Couzens, Amber L., Aman, Ahmed, Gingras, Anne-Claude, Al-Awar, Rima, Fish, Paul V., Gerstenberger, Brian S., Roberts, Lee, Benn, Caroline L., Grimley, Rachel L., Braam, Mitchell J. S., Rossi, Fabio M. V., Sudol, Marius, Brown, Peter J., Bunnage, Mark E., Owen, Dafydd R., Zaph, Colby, Vedadi, Masoud, Arrowsmith, Cheryl H.
Formato: Artigo
Idioma:Inglês
Publicado em: National Academy of Sciences 2014
Assuntos:
Biological Sciences
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4156762/
https://ncbi.nlm.nih.gov/pubmed/25136132
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1073/pnas.1407358111
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