# PSMA-targeted AuNPs for MR guided radiotherapy and radiosensitization

> **NIH NIH R01** · CASE WESTERN RESERVE UNIVERSITY · 2022 · $647,930

## Abstract

Clinical radiation therapy is a noninvasive means to mitigate cancer progression, which is prescribed for
more than 50% of prostate cancer patients. Development of radiation technology, such as utilizing intensity-
modulated radiotherapy (IMRT) to deliver highly conformal radiation dose distributions and image-guided
radiotherapy (IGRT) to account for daily changes in target anatomy and positioning, allows unprecedented levels
of accuracy and therapy outcome. The prostate is surrounded by many nerves and muscle fibers controlling
different excretory and erectile functions that are difficult but necessary to avoid, it still remains a challenge to
precisely deliver radiation doses to prostate cancer without damaging the normal surrounding tissues even with
image guidance. To avoid excessive irradiation doses, radiosensitizers have been developed to amplify the
effects of radiation within tumor cells. Prostate cancer targeted radiosensitizers may offer a means for further
relative biological dose escalation with sparing of normal tissue. However, there has been limited preclinical and
clinical investigation of targeted radiosensitizers for prostate cancer. To address the challenge, we aim to
develop a nanoparticle technology that will improve prostate cancer tissue visualization and discrimination by
MRI, allowing greater accuracy in MRI-guided radiation therapy, and provide radiosensitization within the cancer
cells.
 Prostate specific membrane antigen (PSMA) is an ideal target to detect prostate cancer due to its
abundant expression in most prostate cancers. We have synthesized a novel high-affinity ligand for PSMA
targeting, and conjugated both targeting ligand and Gd(III) complex to gold nanoparticles and nanoclusters
(AuNP/NCs). We have demonstrated that these PSMA-targeted AuNP/NC-Gd(III) have a much higher relaxivity
than free Gd(III) agents and the NP/NCs can be selectively delivered to PSMA-expressing prostate tumor cells,
providing MR image-guided radiation therapy. By delivering Gd(III) conjugated AuNP/NCs directly to prostate
cancer cells we will 1) concentrate the Gd(III) agent to the nanoparticle surface while simultaneously calibrating
the delivery of more Gd(III) agent to target tissues and less of the agent to non-specific or off-target sites; 2)
improve r1 relaxivity and MR sensitivity, which potentially can reduce the given doses to patients and potentially
toxicity of Gd(III) agents; 3) discriminate among cancerous, normal, neural, and muscle cells and tissues with
MRI, enabling precise diagnosis of prostate cancer and precision radiation therapy; 4) combine gold and
gadolinium together to enhance the radiosensitizing effect for potential ablation of prostate cancer using a lower
radiation dose; and 5) enable MRI-guided radiotherapy using MRI LINAC device to enhance radiation accuracy
and avoid collateral damage to normal tissues. We believe that this approach will impact the quality and success
of radiotherapy. Further, PSMA is ...

## Key facts

- **NIH application ID:** 10358618
- **Project number:** 5R01CA260847-02
- **Recipient organization:** CASE WESTERN RESERVE UNIVERSITY
- **Principal Investigator:** BULENT AYDOGAN
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2022
- **Award amount:** $647,930
- **Award type:** 5
- **Project period:** 2021-03-01 → 2025-02-28

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10358618

## Citation

> US National Institutes of Health, RePORTER application 10358618, PSMA-targeted AuNPs for MR guided radiotherapy and radiosensitization (5R01CA260847-02). Retrieved via AI Analytics 2026-05-24 from https://api.ai-analytics.org/grant/nih/10358618. Licensed CC0.

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