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Cryptophane-Folate Biosensor for 129Xe NMR

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Univ Pennsylvania Philadelphia United States

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Folate-conjugated cryptophane was developed for targeting cryptophane to membrane-bound folate receptors that are overexpressed in many human cancers. The cryptophane biosensor was synthesized in 20 nonlinear steps, which included functionalization with folate recognition moiety, solubilizing peptide, and Cy3 fluorophore. Hyperpolarized 129Xe NMR studies confirmed xenon binding to the folate-conjugated cryptophane. Cellular internalization of biosensor was monitored by confocal laser scanning microscopy and quantified by flow cytometry. Competitive blocking studies confirmed cryptophane endocytosis through a folate receptor-mediated pathway. Flow cytometry revealed 10-fold higher cellular internalization in KB cancer cells overexpressing folate receptors compared to HT-1080 cells with normal folate receptor expression. The biosensor was determined to be nontoxic in HT-1080 and KB cells by MTT assay at low micromolar concentrations typically used for hyperpolarized 129Xe NMR experiments.

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Journal Article

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Bionjugate Chemistry , 26, 1, 01 Jan 0001, 01 Jan 0001, Open Access: Publishers Version. May be placed on public websites; ACS AuthorChoice License, which permits copying and redistribution of the article or any adaptations for non-commercial purposes.



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Approved For Public Release;

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