Ontology highlight
ABSTRACT:
SUBMITTER: Remillard D
PROVIDER: S-EPMC6792166 | biostudies-literature | 2019 Oct
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20190913 10
Recent reports have highlighted the dual bromodomains of TAF1 (TAF1(1,2)) as synergistic with BET inhibition in cellular cancer models, engendering interest in TAF/BET polypharmacology. Here, we examine structure activity relationships within the BI-2536 PLK1 kinase inhibitor scaffold, previously reported to bind BRD4. We examine binding by this ligand to TAF1(2) and apply structure guided design strategies to discriminate binding to both the PLK1 kinase and BRD4(1) bromodomain while retaining a ...[more]