Mechanisms of action and resistance in histone methylation-targeted therapy. (https://pubmed.ncbi.nlm.nih.gov/38383791/)

These scientists wanted to understand how a new drug called valemetostat could help treat a type of cancer called adult T cell leukaemia/lymphoma. They studied how this drug works on the cells of patients with this cancer. They found that valemetostat reduced the size of tumours and helped patients get better.

The scientists looked closely at the cells and found that valemetostat affects a part of the cell called chromatin, which controls how genes are turned on and off. By targeting a specific part of chromatin called H3K27me3, the drug was able to stop the cancer cells from growing.

However, they also discovered that some cancer cells became resistant to the drug after a long time. These cells changed in a way that made them harder to treat. The scientists found that mutations in certain genes caused this resistance.

Overall, the scientists learned that targeting specific parts of the cell's chromatin can be a promising way to treat cancer, but they also need to find ways to overcome resistance that may develop over time.

Yamagishi M., Kuze Y., Kobayashi S., Nakashima M., Morishima S., Kawamata T., Makiyama J., Suzuki K., Seki M., Abe K., Imamura K., Watanabe E., Tsuchiya K., Yasumatsu I., Takayama G., Hizukuri Y., Ito K., Taira Y., Nannya Y., Tojo A., Watanabe T., Tsutsumi S., Suzuki Y., Uchimaru K. Mechanisms of action and resistance in histone methylation-targeted therapy. Nature. 2024 Feb 21. doi: 10.1038/s41586-024-07103-x.