Paterson Group Honours Projects

 Supervisor: A/Prof Brett Paterson

Targeted radiopharmaceutical therapy is the use of radioactive molecules to selectively deliver a cytotoxic amount of ionising radiation to treat cancer. The highly ionising alpha (a)  particles produce lethal DNA double strand breaks within the cell nucleus while reducing the amount of unwanted radiation to surrounding tissues.

Lead-212 (²¹²Pb) is the longer-lived parent radionuclide of the short-lived a emitter bismuth-212 (²¹²Bi), and therefore can serve as an in vivo generator of a particles. Tetraazamacrocyclic chelators form stable complexes with ²¹²Pb, however, loss of ²¹²Bi is unfortunately still observed, which can result in damaging off-target effects.

This project involves the synthesis of new chelators for stable encapsulation of ²¹²Pb and ²¹²Bi. The non-radioactive Pb²⁺ and Bi³⁺ complexes will be synthesised and characterised using techniques such as ¹H and ¹³C NMR spectroscopy, HPLC and mass spectrometry. Radiochemical techniques will be used to synthesise the ²¹²Pb complexes and assess the retention of ²¹²Bi.

 Supervisor: A/Prof Brett Paterson

Targeted radiopharmaceutical therapy is the use of radioactive molecules to selectively deliver a cytotoxic amount of ionising radiation to treat cancer. The highly ionising alpha (a) particles produce lethal DNA double strand breaks within the cell nucleus while reducing the amount of unwanted radiation to surrounding tissues.

Lead-212 (²¹²Pb) is the longer-lived parent radionuclide of the short-lived a emitter bismuth-212 (²¹²Bi), and therefore can serve as an in vivo generator of a particles. Tetraazamacrocycles form stable complexes with ²¹²Pb, however the bifunctional linker chemistry that allows them to be efficiently and reliably attached to targeting molecules is limited.

This project involves the solid-phase synthesis of bifunctional chelators for attachment to peptides and proteins for targeting and treating cancer. Radiochemical techniques will be used to synthesise the ²¹²Pb complexes and the radiopharmaceuticals will be assessed in vitro for targeted cytotoxicity of cancer cells.