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Anticancer Agents Med Chem ; 17(10): 1434-1440, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28270070

RESUMO

BACKGROUND: Targeted imaging and therapy (theranostics) is a promising approach for the simultaneous improvement of cancer diagnosis, prognosis and management. Therapeutic and imaging reagents are coupled to tumor-targeting molecules such as antibodies, providing a basis for truly personalized medicine. However, the development of antibody-drug conjugates with acceptable pharmaceutical properties is a complex process and several parameters must be optimized, such as the controlled conjugation method and the drug-to-antibody ratio. OBJECTIVE: The major aim of this work is to address fundamental key challenges for the development of versatile technology platform for generating homogenous immunotheranostic reagent. METHOD: We conjugated the theranostics reagent IRDye700dx to a recombinant antibody fusion protein containing a self-labeling protein (SNAP-tag) which provides a unique reaction site. RESULTS: The resulting conjugate was suitable for the imaging of cancer cells expressing the epidermal growth factor receptor and demonstrated potent phototherapeutic and imaging activities against them. CONCLUSION: Here, we describe a simple, rapid and robust site-directed labeling method that can be used to generate homogeneous immunoconjugate with defined pharmacological properties.


Assuntos
Anticorpos/uso terapêutico , Neoplasias/tratamento farmacológico , Nanomedicina Teranóstica , Anticorpos/química , Relação Dose-Resposta a Droga , Receptores ErbB/análise , Receptores ErbB/biossíntese , Humanos , Indóis/química , Indóis/uso terapêutico , Estrutura Molecular , Compostos de Organossilício/química , Compostos de Organossilício/uso terapêutico , Fotoquimioterapia , Relação Estrutura-Atividade
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