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PLoS One ; 8(3): e58866, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-23554944

RESUMO

Soricidin is a 54-amino acid peptide found in the paralytic venom of the northern short-tailed shrew (Blarina brevicauda) and has been found to inhibit the transient receptor potential of vallinoid type 6 (TRPV6) calcium channels. We report that two shorter peptides, SOR-C13 and SOR-C27, derived from the C-terminus of soricidin, are high-affinity antagonists of human TRPV6 channels that are up-regulated in a number of cancers. Herein, we report molecular imaging methods that demonstrate the in vivo diagnostic potential of SOR-C13 and SOR-C27 to target tumor sites in mice bearing ovarian or prostate tumors. Our results suggest that these novel peptides may provide an avenue to deliver diagnostic and therapeutic reagents directly to TRPV6-rich tumors and, as such, have potential applications for a range of carcinomas including ovarian, breast, thyroid, prostate and colon, as well as certain leukemia's and lymphomas.


Assuntos
Peptídeos/metabolismo , Canais de Cátion TRPV/metabolismo , Animais , Linhagem Celular Tumoral , Feminino , Corantes Fluorescentes , Expressão Gênica , Células HEK293 , Humanos , Imageamento por Ressonância Magnética , Masculino , Camundongos , Conformação Molecular , Imagem Molecular , Neoplasias/diagnóstico , Neoplasias/metabolismo , Ressonância Magnética Nuclear Biomolecular , Imagem Óptica , Peptídeos/química , Canais de Cátion TRPV/antagonistas & inibidores , Canais de Cátion TRPV/genética , Transplante Heterólogo
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