5 years ago

Development of High-Throughput Screening Assays for Inhibitors of ETS Transcription Factors

X.-H., S. L., Bearss, Warner, S., H., Vankayalapati, Currie, D. J., Liu, Sharma, B. J., Graves
ETS transcription factors from the ERG and ETV1/4/5 subfamilies are overexpressed in the majority of prostate cancer patients and contribute to disease progression. Here, we develop two in vitro assays for the interaction of ETS transcription factors with DNA that are amenable for high throughput screening. Using ETS1 as a model, these assays were applied to screen 110 compounds derived from a high-throughput virtual screen. We find that the use of lower affinity DNA-binding sequences, similar to those which ERG and ETV1 bind to in prostate cells, allowed for higher inhibition from many of these test compounds. Further pilot experiments demonstrated that the in vitro assays are robust for ERG, ETV1, and ETV5, three of the ETS transcription factors that are overexpressed in prostate cancer.

Publisher URL: http://biorxiv.org/cgi/content/short/181420v1

DOI: 10.1101/181420

You might also like
Discover & Discuss Important Research

Keeping up-to-date with research can feel impossible, with papers being published faster than you'll ever be able to read them. That's where Researcher comes in: we're simplifying discovery and making important discussions happen. With over 19,000 sources, including peer-reviewed journals, preprints, blogs, universities, podcasts and Live events across 10 research areas, you'll never miss what's important to you. It's like social media, but better. Oh, and we should mention - it's free.

  • Download from Google Play
  • Download from App Store
  • Download from AppInChina

Researcher displays publicly available abstracts and doesn’t host any full article content. If the content is open access, we will direct clicks from the abstracts to the publisher website and display the PDF copy on our platform. Clicks to view the full text will be directed to the publisher website, where only users with subscriptions or access through their institution are able to view the full article.