Ontology highlight
ABSTRACT:
SUBMITTER: Hilinski MK
PROVIDER: S-EPMC3331937 | biostudies-literature | 2012 May
REPOSITORIES: biostudies-literature
Hilinski Michael K MK Mrozowski Roman M RM Clark David E DE Lannigan Deborah A DA
Bioorganic & medicinal chemistry letters 20120313 9
The Ser/Thr protein kinase, RSK, is important in the etiology of tumor progression including invasion and motility. The natural product kaempferol-3-O-(3″,4″-di-O-acetyl-α-l-rhamnopyranoside), called SL0101, is a highly specific RSK inhibitor. Acylation of the rhamnose moiety is necessary for high affinity binding and selectivity. However, the acetyl groups can be cleaved by esterases, which accounts for the poor in vitro biological stability of SL0101. To address this problem a series of analog ...[more]