A novel 18F-labeled brain penetrant PET ligand for imaging poly(ADP-ribose) polymerase-1
Patel, J. S.; Zhou, X.; Chen, J.; Gao, Y.; Zhao, C.; Song, Z.; Zhao, T.; Hu, Q.; Li, X.; Li, C.; Wu, S.; Schuster, D. M.; Yang, L.; Li, Y.; Yu, D. S.; Liang, S. H.
Show abstract
Poly(ADP-ribose) polymerase-1 (PARP-1) is a key mediator of DNA repair, and its inhibition has become a validated therapeutic strategy in homologous recombination-deficient cancers. However, tools for non-invasive assessment of PARP-1-specific expression remain limited. Here, we evaluated [18F]AZD9574, a next-generation PARP-1-selective PET radiotracer. [18F]AZD9574 was tested in a panel of breast, glioblastoma, prostate, and pancreatic cancer cell lines. Uptake correlated with PARP-1 expression and was dose-dependently blocked by a variety of clinically relevant PARP inhibitors, confirming its binding specificity. In 22Rv1 xenograft mouse models, the tracer demonstrated significant tumor accumulation that was specific to PARP-1, and ex vivo biodistribution confirmed organ uptake consistent with specific tumor binding and PARP-1 expression. Together, these findings establish [18F]AZD9574 as a promising PARP-1-targeted imaging agent with strong potential for advancing cancer research and therapeutic monitoring.
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