# EGFR-targeted gadolinium contrast agents for enhanced molecular magnetic resonance imaging of tumors

**Authors:** Mengyao Chen, Jing Chen, Xue Ren, Chunping Liu, Chenwu Bai, Xiaoya Wang, Jianli Duan, Shibin Ai, Xinxin Yan, Fan Yang, Xin Liu

PMC · DOI: 10.1016/j.jbc.2025.110992 · 2025-11-29

## TL;DR

This paper introduces a new MRI contrast agent that targets EGFR-positive tumors, improving detection and diagnosis accuracy.

## Contribution

The novel EGFR-targeted gadolinium agents offer enhanced specificity and sensitivity for tumor imaging.

## Key findings

- EBP-Gd conjugates showed high binding affinity and specificity for EGFR-positive cells.
- In vivo studies demonstrated increased tumor uptake and prolonged contrast retention.
- The agents outperformed traditional non-targeted Gd-DO3A in specificity and sensitivity.

## Abstract

Magnetic resonance imaging (MRI) is a widely used tool for tumor diagnosis, but current contrast agents often lack sufficient sensitivity and specificity. To address these limitations, we developed novel gadolinium-based (Gd) contrast agents conjugated with epidermal growth factor receptor (EGFR)-binding peptides (EBPs) for targeted MRI of EGFR-overexpressing tumors. The synthesized EBP-Gd-DO3A and EBP-(Gd-DO3A)3 conjugates exhibited high binding affinity and specificity for EGFR-positive cells, as demonstrated through cell binding assays and fluorescence microscopy. Competitive binding assays confirmed EGFR-mediated specificity. In vitro MRI revealed strong contrast enhancement in EGFR-overexpressing tumor cells, while in vivo studies in xenograft models showed increased tumor uptake and prolonged contrast retention. These agents demonstrated superior specificity and sensitivity compared to traditional non-targeted Gd-DO3A, offering a promising approach for improved tumor detection, grading, and prognosis in clinical molecular imaging.

## Linked entities

- **Genes:** EGFR (epidermal growth factor receptor) [NCBI Gene 1956]
- **Chemicals:** gadolinium (PubChem CID 23982), Gd-DO3A (PubChem CID 60714)

## Full-text entities

- **Genes:** EGFR (epidermal growth factor receptor) [NCBI Gene 1956] {aka ERBB, ERBB1, ERRP, HER1, NISBD2, NNCIS}, EBP (EBP cholestenol delta-isomerase) [NCBI Gene 10682] {aka CDPX2, CHO2, CPX, CPXD, D8D7I, MEND}
- **Diseases:** Tumors (MESH:D009369)
- **Chemicals:** Gadolinium (MESH:D005682)

## Figures

6 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12810539/full.md

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Source: https://tomesphere.com/paper/PMC12810539