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. 2018 Oct 4;19(19):2055-2060.
doi: 10.1002/cbic.201800335. Epub 2018 Sep 14.

Expanding the Applicability of the Metal Labeling of Biomolecules by the RIKEN Click Reaction: A Case Study With Gallium-68 Positron Emission Tomography

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Expanding the Applicability of the Metal Labeling of Biomolecules by the RIKEN Click Reaction: A Case Study With Gallium-68 Positron Emission Tomography

Yuka Nakamoto et al. Chembiochem. .

Abstract

Radiolabeled biomolecules with short half-life times are of increasing importance for positron emission tomography (PET) imaging studies. Herein, we demonstrate an improved and generalized method for synthesizing a [radiometal]-unsaturated aldehyde as a lysine-labeling probe that can be easily conjugated into various biomolecules through the RIKEN click reaction. As a case study, 68 Ga-PET imaging of U87MG xenografted mice is demonstrated by using the 68 Ga-DOTA-RGDyK peptide, which is selective to αV β3 integrins.

Keywords: biomolecules; click chemistry; gallium; positron emission tomography; radiopharmaceuticals.

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