Potent and selective SETDB1 covalent negative allosteric modulator reduces methyltransferase activit...
Potent and selective SETDB1 covalent negative allosteric modulator reduces methyltransferase activity in cells
About this item
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Author / Creator
Uguen, Mélanie , Shell, Devan J. , Silva, Madhushika , Deng, Yu , Li, Fengling , Szewczyk, Magdalena M. , Yang, Ka , Zhao, Yani , Stashko, Michael A. , Norris-Drouin, Jacqueline L. , Waybright, Jarod M. , Beldar, Serap , Rectenwald, Justin M. , Mordant, Angie L. , Webb, Thomas S. , Herring, Laura E. , Arrowsmith, Cheryl H. , Ackloo, Suzanne , Gygi, Steven P. , McGinty, Robert K. , Barsyte-Lovejoy, Dalia , Liu, Pengda , Halabelian, Levon , James, Lindsey I. , Pearce, Kenneth H. and Frye, Stephen V.
Publisher
London: Nature Publishing Group UK
Journal title
Language
English
Formats
Publication information
Publisher
London: Nature Publishing Group UK
Subjects
More information
Scope and Contents
Contents
A promising drug target, SETDB1, is a dual methyl-lysine (Kme) reader and methyltransferase implicated in cancer and neurodegenerative disease progression. To help understand the role of the triple Tudor domain (3TD) of SETDB1, its Kme reader, we first identify a low micromolar potency small molecule ligand, UNC6535, which occupies simultaneously b...
Alternative Titles
Full title
Potent and selective SETDB1 covalent negative allosteric modulator reduces methyltransferase activity in cells
Authors, Artists and Contributors
Author / Creator
Shell, Devan J.
Silva, Madhushika
Deng, Yu
Li, Fengling
Szewczyk, Magdalena M.
Yang, Ka
Zhao, Yani
Stashko, Michael A.
Norris-Drouin, Jacqueline L.
Waybright, Jarod M.
Beldar, Serap
Rectenwald, Justin M.
Mordant, Angie L.
Webb, Thomas S.
Herring, Laura E.
Arrowsmith, Cheryl H.
Ackloo, Suzanne
Gygi, Steven P.
McGinty, Robert K.
Barsyte-Lovejoy, Dalia
Liu, Pengda
Halabelian, Levon
James, Lindsey I.
Pearce, Kenneth H.
Frye, Stephen V.
Identifiers
Primary Identifiers
Record Identifier
TN_cdi_doaj_primary_oai_doaj_org_article_ed8d996137ea4d0e96be716da2a0fdb9
Permalink
https://devfeature-collection.sl.nsw.gov.au/record/TN_cdi_doaj_primary_oai_doaj_org_article_ed8d996137ea4d0e96be716da2a0fdb9
Other Identifiers
ISSN
2041-1723
E-ISSN
2041-1723
DOI
10.1038/s41467-025-57005-3
