| Autor: |
Taylor R. Nicholas, Jingwei Meng, Benjamin M. Greulich, Teresa Stevie Morris, Peter C. Hollenhorst, Irina U. Agoulnik |
| Jazyk: |
angličtina |
| Rok vydání: |
2020 |
| Předmět: |
|
| Zdroj: |
PLoS ONE, Vol 15, Iss 9 (2020) |
| Druh dokumentu: |
article |
| ISSN: |
1932-6203 |
| Popis: |
Aberrant expression of the transcription factor ERG is a key driving event in approximately one-half of all of prostate cancers. Lacking an enzymatic pocket and mainly disordered, the structure of ERG is difficult to exploit for therapeutic design. We recently identified EWS as a specific interacting partner of ERG that is required for oncogenic function. In this study, we aimed to target this specific protein-protein interaction with small molecules. A high-throughput screening (HTS) strategy was implemented to identify potential protein-protein interaction inhibitors. Secondary assays verified the function of several hit compounds, and one lead compound inhibited ERG-mediated phenotypes in prostate cells. This is the first study aimed at targeting the ERG-EWS protein-protein interaction for the development of a small molecule-based prostate cancer therapy. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
|
