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MR Molecular Imaging of Prostate Cancer with a Small Molecular CLT1 Peptide Targeted Contrast Agent
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A computational and experimental study to develop E-selectin targeted peptides for molecular imaging applications.

Ana Carina Fernandes1,2, Mengjiao Liu3, Teresa Sorbo2

  • 1Instituto de Tecnologia Química e Biológica António Xavier, Universidade Nova de Lisboa, Av. da República, 2780-157 Oeiras, Portugal.

Future Medicinal Chemistry
|December 7, 2018
PubMed
Summary

The peptide H2N-P2 demonstrates high specificity and affinity for E-selectin, making it a promising candidate for developing targeted molecular imaging agents for inflamed endothelium.

Keywords:
E-selectinangiogenesismicrobubblemolecular imagingmolecular modellingpeptidesultrasound

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Area of Science:

  • Biomolecular Engineering
  • Molecular Imaging
  • Cell Biology

Background:

  • E-selectin is a cell adhesion molecule significantly overexpressed on endothelial cells during inflammation and angiogenesis.
  • Targeting E-selectin offers a potential strategy for molecular imaging of these pathological conditions.

Purpose of the Study:

  • To evaluate four novel peptides for their binding affinity and specificity to E-selectin.
  • To assess the suitability of the best-performing peptides for developing E-selectin-targeted molecular ultrasound contrast agents.

Main Methods:

  • Computational analysis, surface plasmon resonance, and in vitro cell-based assays were used to characterize peptide-E-selectin interactions.
  • Peptides were conjugated to poly(butyl cyanoacrylate) microbubbles for evaluation as ultrasound probes in cell cultures and explanted arteries.

Main Results:

  • Peptides H2N-P3A5 and Ac-P4 exhibited stronger binding to E-selectin but lower specificity compared to Ac-P1 and H2N-P2.
  • The peptide H2N-P2 demonstrated superior specificity and affinity for E-selectin among the tested candidates.

Conclusions:

  • The peptide H2N-P2 is identified as a highly suitable candidate for the development of E-selectin-targeted molecular imaging agents.
  • This finding supports the potential of H2N-P2 in advancing diagnostic tools for inflammatory and angiogenic diseases.