What Makes RK-251 ‘Smart’?
RK-251 is a prodrug, meaning it is designed to become pharmacologically active after encountering a specific trigger. In this case, that trigger is reactive oxygen species (ROS), highly reactive molecules that are often present at elevated levels in cancer cells. The researchers designed RK-251 to respond to this difference between tumour cells and normal cells. Once the compound encounters sufficiently high ROS levels, it undergoes a chemical reaction that releases NBDHEX, the anticancer component. NBDHEX inhibits glutathione-S-transferase pi (GSTP1), a protein that is overexpressed in many cancer cells and is involved in processes that can help cancer cells survive and resist certain treatments.