Potent and selective SETDB1 covalent negative allosteric modulator reduces methyltransferase activity in cells

Abstract 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 smal...

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Autors principals:	Mélanie Uguen, Devan J. Shell, Madhushika Silva, Yu Deng, Fengling Li, Magdalena M. Szewczyk, Ka Yang, Yani Zhao, Michael A. Stashko, Jacqueline L. Norris-Drouin, Jarod M. Waybright, Serap Beldar, Justin M. Rectenwald, Angie L. Mordant, Thomas S. Webb, Laura E. Herring, Cheryl H. Arrowsmith, Suzanne Ackloo, Steven P. Gygi, Robert K. McGinty, Dalia Barsyte-Lovejoy, Pengda Liu, Levon Halabelian, Lindsey I. James, Kenneth H. Pearce, Stephen V. Frye
Format:	Artigo
Idioma:	Inglês
Publicat:	Nature Portfolio 2025-02-01
Col·lecció:	Nature Communications
Accés en línia:	https://doi.org/10.1038/s41467-025-57005-3
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