Literature Seminar

Targeted alpha therapy represents an underdeveloped area of cancer treatment. Alpha particles have demonstrated a high degree of cytotoxicity, which when harnessed, can be effective at inducing apoptosis in cancer cells. However, due to the low natural abundance of alpha-emitting radioisotopes and their sparsely studied chemistry, Radium-223 is the only FDA approved radioisotope for this purpose. Thorium-227 is a promising alpha-emitting radioisotope that possesses some advantages over Radium-223, including a relatively high natural abundance and more extensive research of the coordination chemistry. To effectively utilize Thorium-227 for targeted alpha therapy, it must be sequestered in a chelator that binds both rapidly and irreversibly in physiological conditions. The Raymond group synthesized a novel chelator that combines design principles of several ligand structures to bind Th(IV). The kinetics and thermodynamics of complexation under physiological conditions were studied to assess the chelator’s potential use for targeted alpha therapy.