The long journey to bring a Myc inhibitor to the clinic

The oncogene Myc is deregulated in the majority of human tumors and drives numerous hallmarks of cancer. Despite its indisputable role in cancer development and maintenance, Myc is still undrugged. Developing a clinical inhibitor for Myc has been particularly challenging owing to its intrinsically disordered nature and lack of a binding pocket, coupled with concerns regarding potentially deleterious side effects in normal proliferating tissues. However, major breakthroughs in the development of Myc inhibitors have arisen in the last couple of years. Notably, the direct Myc inhibitor that we developed has just entered clinical trials. Celebrating this milestone, with this Perspective, we pay homage to the different strategies developed so far against Myc and all of the researchers focused on developing treatments for a target long deemed undruggable.

Automated summary

The oncogene Myc, deregulated in the majority of human tumors, has been a challenging target for drug development due to its disordered nature and lack of binding pocket. Recent breakthroughs have led to the development of Myc inhibitors, with a direct inhibitor currently in clinical trials, marking a significant milestone in the effort to target this previously undrugged gene.