Sunitinib--CLIO conjugate: a VEGFR/PDGFR-targeting active MR probe.
Mol Imaging Biol
; 16(3): 340-9, 2014 Jun.
Article
em En
| MEDLINE
| ID: mdl-24185817
ABSTRACT
PURPOSE:
This study was conducted to evaluate feasibility of sunitinib-CLIO conjugate as a vascular endothelial growth factor receptor/platelet-derived growth factor receptor (VEGFR/PDGFR)-specific magnetic resonance (MR) probe. PROCEDURE VEGFR/PDGFR-targeting MR probe was synthesized by conjugating cross-linked iron-oxide (CLIO) with tyrosine-kinase inhibitor (sunitinib). In VEGFR/PDGFR-positive (U118MG) and VEGFR/PDGFR-negative (HT29) cells and tumor models, conjugate-driven ΔR 2 was estimated, while CLIO was used as control. Prussian-blue staining was performed for quantifying the amount of tumor-binding conjugates.RESULTS:
ΔR 2 between sunitinib-CLIO-treated and non-treated cells was greater in U118MG (mean, 2.1/s) than in HT29 cells (1.0/s). In in vivo study, conjugate induced a greater ΔR 2 in U118MG (11.2/s) than HT29 tumors (5.9/s). Conjugate-induced R 2 changes were not correlated with degree of Gd-DTPA enhancement, demonstrating that tumor binding of sunitinib-CLIO was independent of enhanced permeability and retention effect. % area of Prussian-blue staining was greater in U118MG (8.5 %) than in HT29 (1.4 %).CONCLUSIONS:
Sunitinib-CLIO conjugate can be used as an active MR probe for quantifying VEGFR/PDGFR.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pirróis
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Imageamento por Ressonância Magnética
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Compostos Férricos
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Sondas Moleculares
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Receptores do Fator de Crescimento Derivado de Plaquetas
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Receptores de Fatores de Crescimento do Endotélio Vascular
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Indóis
Tipo de estudo:
Prognostic_studies
Limite:
Humans
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article