Evaluation of GX1 and RGD‑GX1 peptides as new radiotracers for angiogenesis evaluation in experimental glioma models
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Amino Acids
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Gliomas are the most common type among
all central nervous system tumors. The aggressiveness of
gliomas is correlated with the level of angiogenesis and
is often associated with prognosis. The aim of this study
is to evaluate the novel GX1 peptide and the heterodimer
RGD-GX1 radiolabeled with technetium-99m, for angiogenesis
detection in glioma models. Radiolabeling and
radiochemical controls were assessed for both radioconjugates.
In vitro binding studies in glioma tumor cells were
performed, as well as biodistribution in SCID mice bearing
tumor cells, in order to evaluate the biological behavior
and tumor uptake of the radiocomplexes. Blocking
and imaging studies were also conducted. MicroSPECT/
CT images were acquired in animals with experimentally implanted intracranial tumor. Open field activity was
performed to evaluate behavior, as well as perfusion and
histology analysis. The radiochemical purity of both radiotracers
was greater than 96 %. In vitro binding studies
revealed rather similar binding profile for each molecule.
The highest binding was for RGD-GX1 peptide at
120 min in U87MG cells (1.14 ± 0.35 %). Tumor uptake
was also favorable for RGD-GX1 peptide in U87MG
cells, reaching 2.96 ± 0.70 % at 1 h p.i. with 47 % of
blocking. Imaging studies also indicated better visualization
for RGD-GX1 peptide in U87MG cells. Behavior
evaluation pointed brain damage and histology studies
confirmed actual tumor in the uptake site. The results
with the angiogenesis seeking molecule 99mTc-HYNIC-E-
[c(RGDfk)-c(GX1)] were successful, and better than with
99mTc-HYNIC-PEG4-c(GX1). Future studies targeting
angiogenesis in other glioma and nonglioma tumor models
are recommended.
Como referenciar
OLIVEIRA, ERICA A. de; FAINTUCH, BLUMA L.; TARGINO, ROSELAINE C.; MORO, ANA M.; MARTINEZ, RAQUEL C.R.; PAGANO, ROSANA L.; FONOFF, ERICH T.; CARNEIRO, CAMILA de G.; GARCEZ, ALEXANDRE T.; FARIA, DANIELE de P.; BUCHPIGUEL, CARLOS A. Evaluation of GX1 and RGD‑GX1 peptides as new radiotracers for angiogenesis evaluation in experimental glioma models. Amino Acids, v. 48, n. 3, p. 821-831, 2016. DOI: 10.1007/s00726-015-2130-y. Disponível em: http://repositorio.ipen.br/handle/123456789/27701. Acesso em: 30 Dec 2025.
Esta referência é gerada automaticamente de acordo com as normas do estilo IPEN/SP (ABNT NBR 6023) e recomenda-se uma verificação final e ajustes caso necessário.