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Bioorg Med Chem Lett ; 21(8): 2550-3, 2011 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-21392985

RESUMO

EGFR is over-expressed in several solid tumors including breast, prostate, pancreas, and lung cancers and is correlated to the metastatic potential of the tumor. Anti-EGFR receptor-binding peptidomimetics (AERP) were examined to assess the small molecule's potential use as tumor-specific imaging agents. The aim of this work was to design and characterize the binding specificity of the radiolabeled peptidomimetics to EGFR over-expressing cell lysate and to A431 xenograft tumors. Our newly designed peptidomimetic, AERP, was conjugated to DTPA and labeled with (99m)Tc. The in vivo tumor accumulation of [(99m)Tc] DTPA-AERP-2 was 1.6±0.1%ID/g and tumor to muscle ratio was 5.5. Our studies suggest that this novel peptidomimetic, AERP-2, warrants further development as an EGFR specific tumor-imaging agent.


Assuntos
Inibidores Enzimáticos/química , Receptores ErbB/antagonistas & inibidores , Neoplasias/diagnóstico por imagem , Compostos Radiofarmacêuticos/química , Animais , Linhagem Celular Tumoral , Inibidores Enzimáticos/síntese química , Receptores ErbB/metabolismo , Humanos , Camundongos , Camundongos Nus , Ácido Pentético/química , Peptidomiméticos , Cintilografia , Compostos Radiofarmacêuticos/síntese química , Tecnécio/química , Distribuição Tecidual , Transplante Heterólogo
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