Ontology highlight
ABSTRACT:
SUBMITTER: Hu L
PROVIDER: S-EPMC3648997 | biostudies-literature | 2013 May
REPOSITORIES: biostudies-literature
Bioorganic & medicinal chemistry letters 20130314 10
A high-throughput screen (HTS) of the MLPCN library using a homogenous fluorescence polarization assay identified a small molecule as a first-in-class direct inhibitor of Keap1-Nrf2 protein-protein interaction. The HTS hit has three chiral centers; a combination of flash and chiral chromatographic separation demonstrated that Keap1-binding activity resides predominantly in one stereoisomer (SRS)-5 designated as ML334 (LH601A), which is at least 100× more potent than the other stereoisomers. The ...[more]