# Brain Penetrant PARP Targeted PET Imaging Probes

> **NIH NIH R03** · YALE UNIVERSITY · 2021 · $82,825

## 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 organization:** YALE UNIVERSITY
- **Principal Investigator:** Zhengxin Cai
- **Activity code:** R03 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $82,825
- **Award type:** 3
- **Project period:** 2020-04-01 → 2022-09-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10287654

## Citation

> US National Institutes of Health, RePORTER application 10287654, Brain Penetrant PARP Targeted PET Imaging Probes (3R03CA249569-02S1). Retrieved via AI Analytics 2026-05-28 from https://api.ai-analytics.org/grant/nih/10287654. Licensed CC0.

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