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Targeting TMPRSS2-ERG in Prostate Cancer

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Technical Report,01 Sep 2014,31 Aug 2015

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Dana Farber Cancer Institute Boston United States

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About half of all prostate cancers are known to harbor a genetic mutation that fuses a gene known as ERG to the regulatory region of thegene TMPRSS2. The TMPRSS2-ERG fusion results in ERG becoming aberrantly activated in prostate cells, which contributes to thedevelopment of cancer. However, despite being an attractive and logical therapeutic target, there are currently no drugs that target ERGactivity. ERG belongs to a group of proteins known as transcription factors, which have been historically difficult for drug developmentbecause they lack the well characterized active sites of enzymes in which to fit small molecule inhibitors. To address these challenges, wedeveloped a method to measure gene expression patterns in a high throughput format and generated a gene signature that differentiatesbetween cells that have active TMPRSS2-ERG activity versus cells in which its activity is suppressed. By using a gene signature as asurrogate for biological activity, we have developed an accurate readout for TMPRSS2-ERG activity. We applied this technique to screengenetic and chemical libraries to study ERG mediated tumorigenesis and identify novel therapeutic agents targeting ERG activity.

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