Dataset Information
LC-MS/MS of SETDB1 3TD after incubation with covalent ligands
Ontology highlight
ABSTRACT:
INSTRUMENT(S): Q Exactive HF
ORGANISM(S): Homo Sapiens (human)
SUBMITTER: 
Melanie Uguen
LAB HEAD: Laura Herring
PROVIDER: PXD056206 | Pride | 2025-05-07
REPOSITORIES: Pride
Dataset's files
Items per page: 1 - 5 of 19 |
Publications
Potent and selective SETDB1 covalent negative allosteric modulator reduces methyltransferase activity in cells.
Nature communications 20250224 1
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 both the TD2 and TD3 reader binding sites. Further optimization leads to the discovery of UNC10013, a covalent 3TD ligand targeting Cys385 of SETDB1. U ...[more]
