# Biocompatible Magnetic Resonance Probes for in vivo Concurrent Profiling

> **NIH NIH R00** · WEST VIRGINIA UNIVERSITY · 2021 · $237,804

## Abstract

PROJECT SUMMARY/ABSTRACT
Cancer research has recently experienced a paradigm shift from the seemingly obvious target of tumor cells
towards key support systems of cancer, such as the tumor microenvironment (TME). Tissue oxygenation (pO2)
and acidosis (pH) are among the most established hallmarks in solid tumor. Recently, extracellular inorganic
phosphate (Pi) has been identified as a new signaling molecule of importance in tumorigenesis. This project
aims to develop new biocompatible paramagnetic probes suitable for systemic delivery allowing for in vivo
concurrent measurement of tissue acidosis (pH), oxygenation (pO2) and Pi concentration in the extracellular
compartment (HOPE probes) using electron paramagnetic resonance (EPR)-based technologies. These
developments will provide a new unique tool in cancer research allowing for in vivo direct non-invasive
measurements and correlation of these important TME parameters. Under SA1, a robust click chemistry
approach has been designed to efficiently produce a library of PEGylated HOPE probes. Under SA2, tumor
targeting will be achieved upon conjugation of the PEGylated probe to RGD and/or folic acid ligands. The
synthesized probes will be evaluated in vitro for their functional sensitivity, spectral properties, toxicity and
ability to bind to the targeted biological receptors. Finally, under SA3, we will use a mouse model of human
breast cancer to perform toxicokinetic studies, to optimize the probe dose and experimental time window, and
to determine the functional sensitivity and tumor targeting efficiency of the probes using low frequency EPR
spectroscopy and Overhauser-enhanced magnetic resonance imaging. We anticipate to achieve in vivo
functional sensitivity of 1-2 mmHg of pO2, 0.05 units of pH, and 0.1 mM of Pi. We expect the dual targeted
approach of the two receptors upregulated in numerous cancer types to improve the contrast between healthy
and tumor tissues, and to significantly enhance signal intensity and decrease probe dosage. The completion
of this K99/R00 award by the PI will allow him to obtain the necessary tools and skills in EPR-based in vivo
spectroscopy and imaging to successfully apply this knowledge to the field of cancer functional imaging;
therefore, bridging the interface between synthetic organic chemistry, cancer research and imaging
technologies. The successful completion of this project is designed to make a signficant impact on the future
of bioimaging applications to medicine.

## Key facts

- **NIH application ID:** 10180962
- **Project number:** 5R00EB023990-05
- **Recipient organization:** WEST VIRGINIA UNIVERSITY
- **Principal Investigator:** Benoit Driesschaert
- **Activity code:** R00 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $237,804
- **Award type:** 5
- **Project period:** 2019-08-01 → 2024-04-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10180962

## Citation

> US National Institutes of Health, RePORTER application 10180962, Biocompatible Magnetic Resonance Probes for in vivo Concurrent Profiling (5R00EB023990-05). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/10180962. Licensed CC0.

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