(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells
(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells
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Author / Creator
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 and Arrowsmith, Cheryl H.
Publisher
United States: National Academy of Sciences
Journal title
Language
English
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Publication information
Publisher
United States: National Academy of Sciences
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Scope and Contents
Contents
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 ᵢᵃᵖᵖ = 0.33 nM), selective, and cell-active inhibitor of the methyltransferase activity of human SETD7—and i...
Alternative Titles
Full title
(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells
Authors, Artists and Contributors
Author / Creator
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.
Identifiers
Primary Identifiers
Record Identifier
TN_cdi_crossref_citationtrail_10_1073_pnas_1407358111
Permalink
https://devfeature-collection.sl.nsw.gov.au/record/TN_cdi_crossref_citationtrail_10_1073_pnas_1407358111
Other Identifiers
ISSN
0027-8424
E-ISSN
1091-6490
DOI
10.1073/pnas.1407358111
