Imaging poly(ADP-ribose) polymerase-1 (PARP1) <i>in vivo</i> with ¹⁸F-labeled brain penetrant positron emission tomography (PET) ligand.

ABSTRACT: Poly(ADP-ribose) polymerase 1 (PARP1) is a multifunctional protein involved in diverse cellular functions, notably DNA damage repair. Pharmacological inhibition of PARP1 has therapeutic benefits for various pathologies. Despite the increased use of PARP inhibitors, challenges persist in achieving PARP1 selectivity and effective blood-brain barrier (BBB) penetration. The development of a PARP1-specific positron emission tomography (PET) radioligand is crucial for understanding disease biology and performing target occupancy studies, which may aid in the development of PARP1-specific inhibitors. In this study, we leverage the recently identified PARP1 inhibitor, AZD9574, to introduce the design and development of its ¹⁸F-isotopologue ([¹⁸F]AZD9574). Our comprehensive ap

SUBMITTER: Zhou X 

PROVIDER: S-EPMC12541583 | biostudies-literature | 2025 Oct

REPOSITORIES: biostudies-literature