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

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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Main Authors: 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: Article
Language:English
Published: Nature Portfolio 2025-02-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-025-57005-3
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