| Texto completo | |
| Autor(es): |
Mendonca, Fernanda Ferreira
;
Sobral, Danielle Vieira
;
Durante, Ana Claudia Ranucci
;
Miranda, Ana Claudia Camargo
;
Mejia, Jorge
;
Faria, Daniele de Paula
;
Marques, Fabio Luiz Navarro
;
de Barboza, Marycel Figols
;
Fuscaldi, Leonardo Lima
;
Malavolta, Luciana
Número total de Autores: 10
|
| Tipo de documento: | Artigo Científico |
| Fonte: | Amino Acids; v. 56, n. 1, p. 13-pg., 2024-01-29. |
| Resumo | |
Breast cancer remains a pressing public health issue primarily affecting women. Recent research has spotlighted bioactive peptides derived from laminin-111, implicated in breast tumor development. Remarkably, the sequences IKVAV, YIGSR, and KAFDITYVRLKF from the alpha 1, beta 1, and gamma 1 chains, respectively, have garnered significant attention. This study aims to assess the potential of these radiolabeled peptides as targeting agents for breast cancer. The three peptides were synthesized using the Fmoc strategy, purified via reversed-phase high-performance liquid chromatography (RP-HPLC), and characterized through mass spectrometry. Iodine-131 (131I) radiolabeling was performed using the chloramine T method, exhibiting high radiochemical yield and stability for [131I]I-YIKVAV and [131I]I-YIGSR. Conversely, [131I]I-KAFDITYVRLKF demonstrated low radiochemical yield and stability and was excluded from the biological studies. The lipophilicity of the compounds ranged from - 2.12 to - 1.10. Serum protein binding assay for [131I]I-YIKVAV and [131I]I-YIGSR reached approximately equal to 48% and approximately equal to 25%, respectively. Affinity for breast cancer cells was evaluated using MDA-MB-231 and MCF-7 tumor cell lines, indicating the affinity of the radiopeptides with these tumor cells. Ex vivo biodistribution profiles of the radiopeptides were assessed in the MDA-MB-231 breast tumor animal model, revealing tumor tissue accumulation, supported by a high tumor-to-contralateral muscle ratio and autoradiography. These results signify the effective penetration of YIKVAV and YIGSR into tumor tissue. Therefore, the synthesized alpha 1 and beta 1 peptide fragments exhibit favorable characteristics as potential breast cancer-targeting agents, promising future exploration as radiopharmaceuticals for breast cancer. (AU) | |
| Processo FAPESP: | 21/08717-8 - Síntese de complexos de cobre, prata e ouro envolvendo análogos de nucleotídeos na busca por novas alternativas para o tratamento do câncer de ovário |
| Beneficiário: | Pedro Paulo Corbi |
| Modalidade de apoio: | Auxílio à Pesquisa - Regular |