| First Author | Jing H | Year | 2016 |
| Journal | Cancer Cell | Volume | 29 |
| Issue | 3 | Pages | 297-310 |
| PubMed ID | 26977881 | Mgi Jnum | J:231764 |
| Mgi Id | MGI:5774902 | Doi | 10.1016/j.ccell.2016.02.007 |
| Citation | Jing H, et al. (2016) A SIRT2-Selective Inhibitor Promotes c-Myc Oncoprotein Degradation and Exhibits Broad Anticancer Activity. Cancer Cell 29(3):297-310 |
| abstractText | Targeting sirtuins for cancer treatment has been a topic of debate due to conflicting reports and lack of potent and specific inhibitors. We have developed a thiomyristoyl lysine compound, TM, as a potent SIRT2-specific inhibitor with a broad anticancer effect in various human cancer cells and mouse models of breast cancer. Mechanistically, SIRT2 inhibition promotes c-Myc ubiquitination and degradation. The anticancer effect of TM correlates with its ability to decrease c-Myc level. TM had limited effects on non-cancerous cells and tumor-free mice, suggesting that cancer cells have an increased dependency on SIRT2 that can be exploited for therapeutic benefit. Our studies demonstrate that SIRT2-selective inhibitors are promising anticancer agents and may represent a general strategy to target certain c-Myc-driven cancers. |
