Active Targeting of Tumors through Conformational Epitope Imprinting |
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Authors: | Yan Zhang Chunyue Deng Sha Liu Jin Wu Prof Dr Zhangbao Chen Prof Dr Chong Li Prof Weiyue Lu |
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Institution: | 1. Key Laboratory of Luminescence and Real‐time Analytical Chemistry (Ministry of Education), College of Pharmaceutical Sciences, Southwest University, No. 2 Tiansheng Road, Beibei, Chongqing 400715 (China);2. Chongqing Engineering Research Center for Pharmaceutical Process and Quality Control (China);3. Key Laboratory of Smart Drug Delivery (Ministry of Education), School of Pharmacy, Fudan University, Shanghai 201203 (China) |
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Abstract: | Inspired by the knowledge that most antibodies recognize a conformational epitope because of the epitope’s specific three‐dimensional shape rather than its linear structure, we combined scaffold‐based peptide design and surface molecular imprinting to fabricate a novel nanocarrier harboring stable binding sites that captures a membrane protein. In this study, a disulfide‐linked α‐helix‐containing peptide, apamin, was used to mimic the extracellular, structured N‐terminal part of the protein p32 and then serve as an imprinting template for generating a sub‐40 nm‐sized polymeric nanoparticle that potently binds to the target protein, recognizes p32‐positive tumor cells, and successfully mediates targeted photodynamic therapy in vivo. This could provide a promising alternative for currently used peptide‐modified nanocarriers and may have a broad impact on the development of polymeric nanoparticle‐based therapies for a wide range of human diseases. |
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Keywords: | conformational epitopes drug delivery imprinting photodynamic therapy tumor targeting |
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