Loading...
Please wait, while we are loading the content...
Small molecule selectively suppresses MYC transcription in cancer cells.
| Content Provider | Semantic Scholar |
|---|---|
| Author | Bouvard, Claire Lim, Sang Min Ludka, John Yazdani, Nahid M. Woods, Ashley K. Chatterjee, Arnab K. Schultz, Peter G. Zhu, Shoutian |
| Copyright Year | 2017 |
| Abstract | Stauprimide is a staurosporine analog that promotes embryonic stem cell (ESC) differentiation by inhibiting nuclear localization of the MYC transcription factor NME2, which in turn results in down-regulation of MYC transcription. Given the critical role the oncogene MYC plays in tumor initiation and maintenance, we explored the potential of stauprimide as an anticancer agent. Here we report that stauprimide suppresses MYC transcription in cancer cell lines derived from distinct tissues. Using renal cancer cells, we confirmed that stauprimide inhibits NME2 nuclear localization. Gene expression analysis also confirmed the selective down-regulation of MYC target genes by stauprimide. Consistent with this activity, administration of stauprimide inhibited tumor growth in rodent xenograft models. Our study provides a unique strategy for selectively targeting MYC transcription by pharmacological means as a potential treatment for MYC-dependent tumors. |
| Starting Page | 3497 |
| Ending Page | 3502 |
| Page Count | 6 |
| File Format | PDF HTM / HTML |
| PubMed reference number | 28292893 |
| Journal | Medline |
| Volume Number | 114 |
| Issue Number | 13 |
| Alternate Webpage(s) | http://www.pnas.org/content/114/13/3497.full.pdf |
| Alternate Webpage(s) | https://doi.org/10.1073/pnas.1702663114 |
| Journal | Proceedings of the National Academy of Sciences of the United States of America |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |