Background: Labeled RGD peptide that specifically targets ανβ3 integrin has great potential
for the early diagnosis of malignant tumors.αvβ3 integrin receptors appear specifically
more on the surface of glioblastoma (malignant glioma) cells rather than normal cells.
Objective: The aim of this study was to identify a novel RGD that can be radiolabeled with99m
with in vitro
assessment of its targeting ability for U87MG human brain cancer cells.
Method: Novel RGD was designed by Amino Acid retro-inversion technique. The peptide HYNIC
conjugate was radiolabeled with 99m
Tc at 95°C for 10 min and radiochemical analysis was performed
using ITLC and HPLC methods. The stability of the radiopeptide was checked in the presence
of human serum at 37°C up to 24 h. Binding properties and internalization were studied with
Results: Novel HYNIC-RGD has shown high radiochemical purity over 98%. Radioconjugate
binding and internalization in U87MG cells were high and specific (13.96% and 12.38% at 4 h respectively).
The radiolabeled peptide revealed good affinity for glioblastoma cells (Kd
Conclusion: The in vitro
study demonstrated the targeting ability of novel 99m
glioblastoma cells. Therefore, more in vivo
studies are required.