Ontology highlight
ABSTRACT:
SUBMITTER: Moustakim M
PROVIDER: S-EPMC6348381 | biostudies-literature | 2018 Dec
REPOSITORIES: biostudies-literature
Angewandte Chemie (International ed. in English) 20181116 50
YEATS domain (YD) containing proteins are an emerging class of epigenetic targets in drug discovery. Dysregulation of these modified lysine-binding proteins has been linked to the onset and progression of cancers. We herein report the discovery and characterisation of the first small-molecule chemical probe, SGC-iMLLT, for the YD of MLLT1 (ENL/YEATS1) and MLLT3 (AF9/YEATS3). SGC-iMLLT is a potent and selective inhibitor of MLLT1/3-histone interactions. Excellent selectivity over other human YD p ...[more]