# Brain Penetrant PARP Targeted PET Imaging Probes

> **NIH NIH R03** · YALE UNIVERSITY · 2021 · $83,750

## Abstract

ABSTRACT
 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 single
strand DNA repair. With multiple ongoing clinical trials using PARPis to treat glioma, to assess baseline PARP
expression levels through quantitative PARP PET imaging will provide prognostic information. However, none of
the current PARP imaging agents under development is brain penetrant, making the reliable quantification of
PARP-1 in brain challenging. Herein, we propose to evaluate a brain penetrant PARP-1 inhibitor and its analogs
as potential PET imaging agents.

## Key facts

- **NIH application ID:** 10128417
- **Project number:** 5R03CA249569-02
- **Recipient organization:** YALE UNIVERSITY
- **Principal Investigator:** Zhengxin Cai
- **Activity code:** R03 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $83,750
- **Award type:** 5
- **Project period:** 2020-04-01 → 2022-09-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10128417

## Citation

> US National Institutes of Health, RePORTER application 10128417, Brain Penetrant PARP Targeted PET Imaging Probes (5R03CA249569-02). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/10128417. Licensed CC0.

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