Potent and Selective SETDB1 Covalent Negative Allosteric Modulator Reduces Methyltransferase Activity in Cells
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, , Stephen V. Frye
The paper identifies UNC10013, a covalent ligand targeting SETDB1's 3TD domain, which reduces methyltransferase activity and shows selectivity in cells.
Nature Communications · Feb 24, 2025Peer-reviewedMolecular Biology