In vitro evaluation and biodistribution of a 99mTc-labeled anti-VEGF peptide targeting neuropilin-1.
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.
Perret
Gérard Y
GY
Ciblage et Imagerie Fonctionnelle de la Progression Tumorale (UPRES 2360), Bobigny, France.
Starzec
Anna
A
Hauet
Nathalie
N
Vergote
Jackie
J
Le Pecheur
Marie
M
Vassy
Roger
R
Léger
Gérard
G
Verbeke
Kristin A
KA
Bormans
Guy
G
Nicolas
Patrick
P
Verbruggen
Alfons M
AM
Moretti
Jean-Luc
JL
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*
D010455:Peptides; D019275:Radiopharmaceuticals; D042461:Vascular Endothelial Growth Factor A; D039942:Neuropilin-1; D013667:Technetium