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- W2263922604 abstract "Two new bifunctional tris(hydroxypyridinone) (THP) chelators designed specifically for rapid labeling with 68Ga have been synthesized, each with pendant isothiocyanate groups and three 1,6-dimethyl-3-hydroxypyridin-4-one groups. Both compounds have been conjugated with the primary amine group of a cyclic integrin targeting peptide, RGD. Each conjugate can be radiolabeled and formulated by treatment with generator-produced 68Ga3+ in over 95% radiochemical yield under ambient conditions in less than 5 min, with specific activities of 60–80 MBq nmol–1. Competitive binding assays and in vivo biodistribution in mice bearing U87MG tumors demonstrate that the new 68Ga3+-labeled THP peptide conjugates retain affinity for the αvβ3 integrin receptor, clear within 1–2 h from circulation, and undergo receptor-mediated tumor uptake in vivo. We conclude that bifunctional THP chelators can be used for simple, efficient labeling of 68Ga biomolecules under mild conditions suitable for peptides and proteins." @default.
- W2263922604 created "2016-06-24" @default.
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- W2263922604 date "2015-09-02" @default.
- W2263922604 modified "2023-10-12" @default.
- W2263922604 title "New Tris(hydroxypyridinone) Bifunctional Chelators Containing Isothiocyanate Groups Provide a Versatile Platform for Rapid One-Step Labeling and PET Imaging with <sup>68</sup>Ga<sup>3+</sup>" @default.
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- W2263922604 doi "https://doi.org/10.1021/acs.bioconjchem.5b00335" @default.
- W2263922604 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/4759618" @default.
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