| Registro completo |
| Provedor de dados: |
BJPS
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| País: |
Brazil
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| Título: |
Synthesis and biological evaluation of 125I-erythropoietin as a potential radiopharmaceutical agent for tumours
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| Autores: |
Clemente,Gonçalo dos Santos
Duarte,Vera Lúcia Serra
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| Data: |
2011-03-01
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| Ano: |
2011
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| Palavras-chave: |
Erythropoietin (EPO)
Glycoprotein hormone
125I-erythropoietin/synthesis
125I-erythropoietin/biological evaluation
Erythropoiesis/regulation
Radiopharmaceuticals
Iodine-125/labelled
EPO expressive tumours
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| Resumo: |
Erythropoietin (EPO) is a glycoprotein hormone responsible for regulating erythropoiesis. Expression of EPO and EPO receptors (EPOr) has recently been demonstrated in some neoplastic cell lines and tumours, suggesting a potential new target for therapy. In this work, EPO was labeled with iodine-125 using the lactoperoxidase method, known to prevent damage to protein during radioiodination, and labeling conditions were optimized. In vitro stability studies have shown that 125I-EPO is radiochemically stable for 20 days after radiolabeling. In vitro cell binding studies have demonstrated very low binding (<2%) of EPO to normal and neoplastic cell lines tested. As expected, the biodistribution in healthy mice exhibited comparatively high rates of fixation in the organs of the excretory system. Thyroid also proved to be a critical organ which may indicate in vivo dissociation of 125I-EPO. In mice with induced melanoma, only a residual fixation in the tumour was evident. Further studies are warranted on other tumoral cell lines to better understand the binding process and internalization into cells. Studies on EPO labeled with carbon-11 could be valuable, since there is a greater chance of preserving the biological activity of the protein using this method.
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| Tipo: |
Info:eu-repo/semantics/article
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| Idioma: |
Inglês
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| Identificador: |
http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502011000100010
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| Editor: |
Universidade de São Paulo, Faculdade de Ciências Farmacêuticas
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| Relação: |
10.1590/S1984-82502011000100010
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| Formato: |
text/html
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| Fonte: |
Brazilian Journal of Pharmaceutical Sciences v.47 n.1 2011
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| Direitos: |
info:eu-repo/semantics/openAccess
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