Identification of Small Molecules Targeting the Posttranscriptional Control of ERG Expression
Abstract
TMPRSS2-ERG translocation is involved in about 60% of prostate cancers. The translocation leads to overexpression of ERG which promotes cell proliferation and abrogates prostate epithelial differentiation. Suppression of ERG expression represents a major way to treat prostate cancers. However, there are no effective means to inhibit ERG expression. Although siRNA can deplete ERG expression, the big challenge is to deliver siRNA into prostate cancer cells. The mRNA stability, translation efficiency and protein stability of ERG are under strict control to maintain the ERG protein level. Here we report the establishment of a cell line which can be used to identify small molecules which inhibit ERG expression by targeting its post-transcriptional process. Using this cell line, we performed high-throughput screening and identified Gambogic acid which suppresses ERG expression in ERG-overexpressing prostate cancer cells.
Document Details
- Document Type
- Technical Report
- Publication Date
- Oct 01, 2012
- Accession Number
- ADA575222
Entities
People
- Yijun Zhu
Organizations
- Northwestern University