Brain Penetrant PARP Targeted PET Imaging Probes

NIH RePORTER · NIH · R03 · $82,825 · view on reporter.nih.gov ↗

Abstract

ABSTRACT of the funded parent grant Because tumor cells can survive chemo/radiation therapies through DNA repairment mediated by poly(ADP- ribose) polymerase-1 (PARP-1). PARP-1 inhibitors (PARPis) alone, or in combination with chemotherapy or radiation therapy, have led to substantial gains in the overall survival of cancer patients, by obstructing PARP- catalyzed single DNA repair. With multiple ongoing clinical trials using PARPis to treat glioma, to quantify baseline PARP expression levels through quantitative PARP PET imaging will provide prognostic information to guide future precision treatment. However, none of the current PARP imaging agents under development is brain penetrant, making reliable in vivo quantification of PARP-1 in the brain challenging. Herein, we propose to evaluate several BBB penetrant PARP-1 inhibitors as potential PET imaging agents.

Key facts

NIH application ID
10287654
Project number
3R03CA249569-02S1
Recipient
YALE UNIVERSITY
Principal Investigator
Zhengxin Cai
Activity code
R03
Funding institute
NIH
Fiscal year
2021
Award amount
$82,825
Award type
3
Project period
2020-04-01 → 2022-09-30