Imaging cancer with PARP inhibitors
Biomarkers of cancer include the PARP family of DNA repair enzymes. One particular member of this family, PARP1, has been targeted with inhibitor drugs as a cancer treatment. However, PARP inhibitor drugs can also be modified with fluorescent or radioactive groups. Because PARP1 enzymes are often present in higher levels in the nuclei of cancer cells, labeled inhibitors of PARP1 can also function as agents for cancer detection. We are developing derivatives of these drugs coupled to fluorescent molecules and radiotracers for the detection and monitoring of cancer.
Project publications:
Salinas, et al. Radioiodinated PARP1 tracers for glioblastoma imaging. EJNMMI Res. 2015 Dec;5(1):123,
Wilson, et al. A one-pot radiosynthesis of [18F]PARPi. J Labelled Comp Radiopharm. 2020 Jul;63(9):419-425.
Wilson, et al. PARP-Targeted auger therapy in p53 mutant colon cancer xenograft mouse models. Mol Pharm. 2021 Sep 6;18(9):3418-3428.
Demetrio de Souza França, et al. Polyethylene glycol 3350 (PEG 3350) as a practical vehicle for rapid reconstitution of PARPi-FL formulations for clinical use. Mol Imaging Biol. 2022 Jul 26.