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The long journey to bring a Myc inhibitor to the clinic
Jonathan R Whitfield1, Laura Soucek1,2,3,4
1Vall d'Hebron Institute of Oncology, Edifici Cellex, Barcelona, Spain.
Abstract:
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.
Insights
The oncogene Myc drives cancer but has been difficult to drug. Recent breakthroughs have led to a direct Myc inhibitor entering clinical trials, offering new hope for cancer treatment.
Area of Science:
- Oncology
- Molecular Biology
- Drug Development
Background:
- The Myc oncogene is frequently deregulated in human cancers, promoting tumor growth and progression.
- Targeting Myc has been challenging due to its disordered structure and lack of a druggable pocket.
- Concerns exist regarding potential side effects of Myc inhibitors in normal proliferating tissues.
Purpose of the Study:
- To review strategies for developing Myc inhibitors.
- To highlight recent advancements in Myc-targeted cancer therapy.
- To celebrate the milestone of a direct Myc inhibitor entering clinical trials.
Main Methods:
- Review of scientific literature on Myc and cancer.
- Analysis of different therapeutic strategies against Myc.
- Discussion of challenges and breakthroughs in Myc inhibitor development.
Main Results:
- Major breakthroughs in Myc inhibitor development have occurred recently.
- A direct Myc inhibitor developed by the authors has entered clinical trials.
- The development of Myc inhibitors represents a significant advancement against a previously undruggable target.
Conclusions:
- Myc remains a critical target in oncology.
- Despite challenges, significant progress has been made in developing Myc inhibitors.
- The initiation of clinical trials for a direct Myc inhibitor marks a new era in cancer therapy.
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