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| Status |
Public on Jul 15, 2014 |
| Title |
Development of peptidomimetic inhibitors of the ERG gene fusion product in prostate cancer (expression) |
| Organism |
Homo sapiens |
| Experiment type |
Expression profiling by array
|
| Summary |
Transcription factors play a key role in the development of diverse cancers, and therapeutically targeting them has remained a challenge. In prostate cancer, the gene encoding the transcription factor ERG is recurrently rearranged and plays a critical role in prostate oncogenesis. Here, we identified a series of peptides that interact specifically with the DNA binding domain of ERG. The most prevalent consensus peptide series matched the tumor suppressor Deleted in Liver Cancer 1 (DLC1). ERG inhibitory peptides and derived peptidomimetics (EIPs) bound with high affinity and specificity leading to proteolytic degradation of ERG. The EIPs attenuated ERG-mediated transcription, chromatin recruitment, protein-protein interactions, cell invasion, and tumor growth. Thus, peptidomimetic targeting of transcription factor fusion products may provide a promising therapeutic strategy for prostate cancer as well as other cancers.
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| Overall design |
ERG genes in VCaP cell were knocked down by siERG or siControls for 48 hrs. Biological replicates: 2 control replicates, 2 experimental replicates. ERG proteins were destablized by RI-EIP1 or RI-muEIP1 for 72 hours. Biological replicates: 2 control replicates, 2 experimental replicates.
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| Contributor(s) |
Wang X, Jing X |
| Citation(s) |
28344039 |
| Submission date |
Jun 30, 2014 |
| Last update date |
Oct 24, 2019 |
| Contact name |
Xiaoju Wang |
| E-mail(s) |
xiaojuw@umich.edu
|
| Phone |
734-763-6056
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| Organization name |
University of Michigan
|
| Street address |
1500 E. Medical Center Drive
|
| City |
Ann Arbor |
| State/province |
MI |
| ZIP/Postal code |
48109 |
| Country |
USA |
| |
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| Platforms (1) |
| GPL4133 |
Agilent-014850 Whole Human Genome Microarray 4x44K G4112F (Feature Number version) |
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| Samples (4)
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| This SubSeries is part of SuperSeries: |
| GSE58975 |
Development of peptidomimetic inhibitors of the ERG gene fusion product in prostate cancer |
|
| Relations |
| BioProject |
PRJNA254032 |
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