Ontology highlight
ABSTRACT:
SUBMITTER: Mrozowski RM
PROVIDER: S-EPMC3601785 | biostudies-literature | 2012 Feb
REPOSITORIES: biostudies-literature
Mrozowski Roman M RM Vemula Rajender R Wu Bulan B Zhang Qi Q Schroeder Benjamin R BR Hilinski Michael K MK Clark David E DE Hecht Sidney M SM O'Doherty George A GA Lannigan Deborah A DA
ACS medicinal chemistry letters 20120201 2
Enhanced activity of the Ser/Thr protein kinase, RSK, is associated with transformation and metastasis, which suggests that RSK is an attractive drug target. The natural product, SL0101 (kaempferol 3-O-(3″,4″-di-O-acetyl-α-L-rhamnopyranoside), has been shown to be a RSK selective inhibitor. However, the Ki for SL0101 is 1 μM with a half-life of less than 30 min <i>in vivo</i>. To identify analogues with improved efficacy we designed a set of analogues based on the crystallographic model of SL010 ...[more]