Rational Design and Synthesis of Peptide-Based Probes for Fibroblast Activation Protein-Targeted Magnetic Resonance and NIR-I/II Fluorescence Imaging of Cancer-Associated Fibroblasts

  • 0Department of Radiology, Xinhua Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200092, China.

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Summary

This summary is machine-generated.

Novel dual-modality imaging probes targeting cancer-associated fibroblasts (CAFs) were developed. These probes enhance visualization of CAFs in gastric cancer, improving diagnostic capabilities.

Area Of Science

  • Biomedical Imaging
  • Molecular Imaging
  • Cancer Diagnostics

Background

  • Cancer-associated fibroblasts (CAFs) expressing fibroblast activation protein (FAP) drive tumor progression and therapy resistance.
  • FAP-targeted molecular imaging is crucial for visualizing and quantifying CAFs in tumors.

Purpose Of The Study

  • To design and synthesize novel dual-modality probes for FAP-targeted imaging in gastric cancer.
  • To evaluate the efficacy of these probes for visualizing CAFs in vivo.

Main Methods

  • Rational design and synthesis of two FAP-targeted probes (FAPtp1<sup>Mn-ICG</sup> and FAPtp2<sup>Mn-ICG</sup>) using FAP-targeted peptides, Mn-NOTA, and indocyanine green (ICG).
  • Integration of magnetic resonance (MR) and near-infrared fluorescence (NIRF) imaging modalities.
  • In vitro specificity and biosafety assays, followed by in vivo imaging in tumor-bearing mice.

Main Results

  • Successful synthesis of FAPtp1<sup>Mn-ICG</sup> and FAPtp2<sup>Mn-ICG</sup>, with FAPtp2<sup>Mn-ICG</sup> showing improved NIRF imaging efficiency due to a polyethylene glycol linker mitigating aggregation-caused quenching (ACQ).
  • Both probes demonstrated high FAP-targeted specificity and biosafety in vitro.
  • In vivo imaging successfully visualized subcutaneous tumors and peritoneal metastases in mice.

Conclusions

  • Developed novel FAP-targeted dual-modality probes for enhanced CAF evaluation in gastric cancer.
  • The polyethylene glycol linker strategy effectively improved probe performance.
  • These probes offer a promising platform for advancing peptide-based molecular imaging in cancer diagnostics.