title: In vitro evaluation and biodistribution of a 99mTc-labeled anti-VEGF peptide targeting neuropilin-1.
abstract: Neuropilins (NRP) are receptors of angiogenic vascular endothelial growth factor (VEGF). Their overexpression was correlated with tumor angiogenesis and growth suggesting that their specific targeting could provide a new marker of tumor progression. Here, we observed in vitro that new (99m)Tc-labeled derivative of anti-VEGF heptapeptide, ATWLPPR, binds to NRP1 but not to NRP2. Our radiotracer is stable up to 24 h in human serum and in cysteine challenge. But, its too low affinity and too fast extraction indicate further improvement to give a successful imaging of tumor in vivo.
authors.affiliation: Ciblage et Imagerie Fonctionnelle de la Progression Tumorale (UPRES 2360), Bobigny, France.
authors.forename: Gérard Y
authors.initials: GY
authors.lastname: Perret
authors.forename: Anna
authors.initials: A
authors.lastname: Starzec
authors.forename: Nathalie
authors.initials: N
authors.lastname: Hauet
authors.forename: Jackie
authors.initials: J
authors.lastname: Vergote
authors.forename: Marie
authors.initials: M
authors.lastname: Le Pecheur
authors.forename: Roger
authors.initials: R
authors.lastname: Vassy
authors.forename: Gérard
authors.initials: G
authors.lastname: Léger
authors.forename: Kristin A
authors.initials: KA
authors.lastname: Verbeke
authors.forename: Guy
authors.initials: G
authors.lastname: Bormans
authors.forename: Patrick
authors.initials: P
authors.lastname: Nicolas
authors.forename: Alfons M
authors.initials: AM
authors.lastname: Verbruggen
authors.forename: Jean-Luc
authors.initials: JL
authors.lastname: Moretti
mesh_terms: D000818:Animals; D001943:Breast Neoplasms / Q000000981:diagnostic imaging* / Q000378:metabolism*; D045744:Cell Line, Tumor; D005260:Female; D006801:Humans; D007553:Isotope Labeling / Q000379:methods; D008297:Male; D008657:Metabolic Clearance Rate; D051379:Mice; D008819:Mice, Nude; D039942:Neuropilin-1 / Q000737:chemistry / Q000378:metabolism*; D009928:Organ Specificity; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D011485:Protein Binding; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000737:chemistry / Q000493:pharmacokinetics; D051381:Rats; D015203:Reproducibility of Results; D012680:Sensitivity and Specificity; D013667:Technetium / Q000737:chemistry / Q000494:pharmacology; D014018:Tissue Distribution; D042461:Vascular Endothelial Growth Factor A / Q000037:antagonists & inhibitors* / Q000378:metabolism*
chemical_list: D010455:Peptides; D019275:Radiopharmaceuticals; D042461:Vascular Endothelial Growth Factor A; D039942:Neuropilin-1; D013667:Technetium