Comparison of two peptide radiotracers for prostate carcinoma targeting
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2012
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Clinics
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OBJECTIVES: Scintigraphy is generally not the first choice treatment for prostate cancer, although successful studies
using bombesin analog radiopeptides have been performed. Recently, a novel peptide obtained using a phage
display library demonstrated an affinity for prostate tumor cells. The aim of this study was to compare the use of a
bombesin analog to that of a phage display library peptide (DUP-1) radiolabeled with technetium-99m for the
treatment of prostate carcinoma. The peptides were first conjugated to S-acetyl-MAG3 with a 6-carbon spacer,
namely aminohexanoic acid.
METHODS: The technetium-99m labeling required a sodium tartrate buffer. Radiochemical evaluation was
performed using ITLC and was confirmed by high-performance liquid chromatography. The coefficient partition
was determined, and in vitro studies were performed using human prostate tumor cells. Biodistribution was
evaluated in healthy animals at various time points and also in mice bearing tumors.
RESULTS: The radiochemical purity of both radiotracers was greater than 95%. The DUP-1 tracer was more
hydrophilic (log P = -2.41) than the bombesin tracer (log P = -0.39). The biodistribution evaluation confirmed this
hydrophilicity by revealing the greater kidney uptake of DUP-1. The bombesin concentration in the pancreas was
greater than that of DUP-1 due to specific gastrin-releasing peptide receptors. Bombesin internalization occurred
for 78.32% of the total binding in tumor cells. The DUP-1 tracer showed very low binding to tumor cells during the
in vitro evaluation, although tumor uptake for both tracers was similar. The tumors were primarily blocked by DUP-
1 and the bombesin radiotracer primarily targeted the pancreas.
CONCLUSION: Further studies with the radiolabeled DUP-1 peptide are recommended. With further structural
changes, this molecule could become an efficient alternative tracer for prostate tumor diagnosis.
Como referenciar
FAINTUCH, BLUMA L.; OLIVEIRA, ERICA A.; NUNEZ, EUTIMIO G.F.; MORO, ANA M.; NANDA, P.K.; SMITH, CHARLES J. Comparison of two peptide radiotracers for prostate carcinoma targeting. Clinics, v. 67, n. 2, p. 163-170, 2012. DOI: 10.6061/clinics/2012(02)12. Disponível em: http://repositorio.ipen.br/handle/123456789/27699. Acesso em: 28 Mar 2024.
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.