Accession Number:

ADA592070

Title:

Synthesis and Evaluation of Novel RSK Inhibitors in a Living Human Breast Model

Descriptive Note:

Annual summary rept. 1 Jul 2012- 30 Jun 2013

Corporate Author:

VIRGINIA UNIV CHARLOTTESVILLE

Personal Author(s):

Report Date:

2013-07-01

Pagination or Media Count:

9.0

Abstract:

The p90 ribosomal S6 kinase RSK family of serinethreonine 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.

Subject Categories:

  • Medicine and Medical Research

Distribution Statement:

APPROVED FOR PUBLIC RELEASE