Design and validation of a bifunctional ligand display system for receptor targeting

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Abstract

Here we developed a bacteriophage display particle designed to serve as a bifunctional entity that can target tumors while delivering an agent. We engineered a chimera phage vector containing a pIII-displayed αv integrins-targeting moiety and a pVIII-displayed streptavidin binding adaptor moiety. By using the chimeric phage particle, targeting of αv integrins on cells in culture and tumor-related blood vessels was shown through different applications, including luminescent quantum dots localization, surface plasmon resonance-based binding detection, and an in vivo tumor model. The strategy validated here will accelerate the discovery and characterization of receptor-ligand binding events in high throughput, and cell-specific delivery of diagnostics or therapeutics to organs of choice without the need for chemical conjugation.

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Chen, L., Zurita, A. J., Ardelt, P. U., Giordano, R. J., Arap, W., & Pasqualini, R. (2004). Design and validation of a bifunctional ligand display system for receptor targeting. Chemistry and Biology, 11(8), 1081–1091. https://doi.org/10.1016/j.chembiol.2004.05.019

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