Article
(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.
Proceedings of the National Academy of Sciences of the United States of America - 2 Sept 2014
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
Abstract excerpt
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 (Ki (app) = 0.33 nM), selective, and cell-active inhibitor...
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