Ontology highlight
ABSTRACT:
SUBMITTER: Wright EB
PROVIDER: S-EPMC8344253 | biostudies-literature | 2021 Dec
REPOSITORIES: biostudies-literature
Wright Eric B EB Fukuda Shinji S Li Mingzong M Li Yu Y O'Doherty George A GA Lannigan Deborah A DA
Journal of enzyme inhibition and medicinal chemistry 20211201 1
Identifying isoform-specific inhibitors for closely related kinase family members remains a substantial challenge. The necessity for achieving this specificity is exemplified by the RSK family, downstream effectors of ERK1/2, which have divergent physiological effects. The natural product, SL0101, a flavonoid glycoside, binds specifically to RSK1/2 through a binding pocket generated by an extensive conformational rearrangement within the RSK N-terminal kinase domain (NTKD). In modelling experime ...[more]