Chemoproteomic discovery of a covalent allosteric inhibitor of WRN helicase. (https://pubmed.ncbi.nlm.nih.gov/38658751/)

These scientists were trying to find a way to treat certain types of cancer, specifically those that have a problem with their DNA repair system. They discovered a new drug called VVD-133214 that can target a protein called WRN helicase, which is important for fixing DNA mistakes.

The drug works by attaching to a specific part of the WRN protein and changing its shape so that it can't do its job properly. This causes a lot of damage to the DNA in cancer cells with faulty repair mechanisms, leading to their death.

The scientists tested this drug on mice and found that it was effective in shrinking tumors in colorectal cancer cells that have this DNA repair issue. They believe that this drug could be a promising treatment for patients with these types of cancers.

In simple terms, the scientists found a new drug that can target a specific protein in cancer cells and make them die, which could help treat certain types of cancer.

Baltgalvis KA., Lamb KN., Symons KT., Wu CC., Hoffman MA., Snead AN., Song X., Glaza T., Kikuchi S., Green JC., Rogness DC., Lam B., Rodriguez-Aguirre ME., Woody DR., Eissler CL., Rodiles S., Negron SM., Bernard SM., Tran E., Pollock J., Tabatabaei A., Contreras V., Williams HN., Pastuszka MK., Sigler JJ., Pettazzoni P., Rudolph MG., Classen M., Brugger D., Claiborne C., Plancher JM., Cuartas I., Seoane J., Burgess LE., Abraham RT., Weinstein DS., Simon GM., Patricelli MP., Kinsella TM. Chemoproteomic discovery of a covalent allosteric inhibitor of WRN helicase. Nature. 2024 May;629(8011):435-442. doi: 10.1038/s41586-024-07318-y. Epub 2024 Apr 24.