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Quenched Zwitterionic Cyclic Arg-Gly-Asp-Containing Pentapeptide Probe for Real-Time Brain Tumor Imaging.

Hyunjin Kim1, Maixian Liu1, Yongdoo Choi1

  • 1Division of Technology Convergence, National Cancer Center, 323 Ilsan-ro, Goyang 10408, Republic of Korea.

Pharmaceutics
|August 29, 2024
PubMed
Summary

A new activatable fluorescence imaging probe, Q-cRGD, precisely targets glioma cells for improved brain cancer surgery. This probe enhances tumor visualization, leading to more complete tumor resection and better patient outcomes.

Keywords:
activatable probebrain cancerimagingnear-infrared fluorescencezwitterionic

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Area of Science:

  • Biomedical Engineering
  • Oncology
  • Medical Imaging

Background:

  • Glioblastoma treatment efficacy relies on complete tumor resection, yet conventional surgery often fails.
  • Accurate delineation of tumor margins from healthy tissue is a significant surgical challenge.
  • Current fluorescence probes can lack specificity, hindering effective intraoperative guidance.

Purpose of the Study:

  • To develop a novel activatable fluorescence imaging probe for precise glioma cell targeting.
  • To enhance intraoperative visualization of brain tumor margins.
  • To improve the accuracy of glioblastoma resection.

Main Methods:

  • Synthesized Q-cRGD probe by conjugating a near-infrared (NIR) dye to a tryptophan quencher via a disulfide linkage with a cRGD ligand.
  • Designed the probe to be activatable via redox-responsive disulfide bond cleavage within target cells.
  • Utilized the zwitterionic nature of NIR dyes to minimize non-specific protein interactions.

Main Results:

  • The activatable Q-cRGD probe demonstrated specific targeting of glioma cells.
  • In vivo fluorescence imaging showed a high tumor-to-background signal ratio (TBR) of 2.65 within 3 hours post-injection.
  • The probe's design minimized non-specific binding, enhancing signal clarity.

Conclusions:

  • The novel activatable Q-cRGD probe shows significant potential for intraoperative imaging-guided brain cancer surgery.
  • This probe offers improved tumor margin delineation compared to existing 'always-on' probes.
  • Q-cRGD facilitates more complete tumor resection, potentially improving glioblastoma patient prognosis.