Synthesis and Evaluation of Novel RSK Inhibitors in a Living Human Breast Model
Abstract
The p90 ribosomal S6 kinase (RSK) family of serine/threonine protein kinases, comprising at least four isoforms (RSKs 1-4), has been shown by our laboratory to be critical for breast cancer cell proliferation (1 3). In 2005 our laboratory reported the first specific inhibitor of RSK, SL0101 (1, Figure 1) (3). SL0101 inhibits RSK in both the breast cancer cell line MCF7 and the normal breast cell line MCF-10A, but only inhibits the proliferation of the breast cancer cell line (1 3). This indicates that breast cancer cells have become dependent on RSK and thus identifies RSK as a potential new target for cancer therapeutics. SL0101, given its exquisite specificity for RSK, is an attractive lead compound for medicinal chemistry efforts aimed at discovering a breast cancer drug that acts by inhibiting RSK.
Document Details
- Document Type
- Technical Report
- Publication Date
- Jul 01, 2013
- Accession Number
- ADA592070
Entities
People
- Michael Hilinski
Organizations
- University of Virginia