Tehran University of Medical Sciences

Science Communicator Platform

Stay connected! Follow us on X network (Twitter):
Share this content! On (X network) By
Novel Gd-Dtpa-Peptide for Targeted Breast Tumor Magnetic Resonance Imaging Publisher Pubmed



Reisi Zargari N1 ; Ebrahimi F2 ; Akhlaghi M3 ; Beiki D2, 3 ; Abdi K4 ; Abbasi MA5 ; Ramezanpour S6 ; Asghari SM7
Authors
Show Affiliations
Authors Affiliations
  1. 1. University Campus II, University of Guilan, Rasht, Iran
  2. 2. Department of Nuclear Pharmacy, School of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  3. 3. Research Center for Nuclear Medicine, Tehran University of Medical Sciences, Tehran, Iran
  4. 4. Department of Radiopharmacy and Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  5. 5. Firoozabadi Hospital Clinical Research Development Unit (FHCRDU), Department of Internal Medicine, School of Medicine, Iran University of Medical Sciences (IUMS), Tehran, Iran
  6. 6. Department of Chemistry, K. N. Toosi University of Technology, Tehran, Iran
  7. 7. Institute of Biochemistry and Biophysics (IBB), University of Tehran, Tehran, Iran

Source: Biomedicine and Pharmacotherapy Published:2024


Abstract

The prevalence of breast cancer underscores the imperative for early diagnosis in guiding treatment decisions. This study introduces a novel contrast agent, Gd-DTPA-VGB3, derived from the peptide VGB3 targeting vascular endothelial growth factor receptor-1 (VEGFR1) and VEGFR2, to enhance the contrast of conventional drug Magnevist in breast tumor MRI. The MRI contrast agent was synthesized on rink amide resin via Fmoc strategy, incorporating amino acids, and coupling to diethylenetriaminepentaacetic acid (DTPA). Gadolinium (Gd)-DTPA-VGB3 displayed specific binding to VEGFR1/2 in a displacement binding assay. Gd-DTPA-VGB3 exhibited minimal cytotoxicity to normal MCF-10 cells while inhibiting 4T1 mammary carcinoma cell proliferation. Compared to Magnevist, Gd-DTPA-VGB3 demonstrated a 2.8-fold increase in contrast-to-noise ratio (CNR) (355 vs. 125). Gd-DTPA-VGB3 exhibited enhanced accumulation in 4T1 tumor-bearing mice, resulting in significant signal intensity improvement. The findings highlight Gd-DTPA-VGB3's specific binding to VEGFRs, substantiating its potential as a candidate for enhancing MRI contrast in breast cancer diagnostics. © 2024
Related Docs
1. Development and Application of Dual-Modality Tumor-Targeting Spions for Precision Breast Cancer Imaging, Biomaterials Advances (2025)
2. Enhanced Antitumor Activity of Lapatinib Against Triple-Negative Breast Cancer Via Loading in Human Serum Albumin, International Journal of Biological Macromolecules (2024)
Experts (# of related papers)
Mehdi Shafee Ardestani (2)