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KMID : 1145520170030020098
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Journal of Radiopharmaceuticals and Molecular Probes
2017 Volume.3 No. 2 p.98 ~ p.102
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Synthesis of 125I-labeled tetrazine for efficient radiolabeling of human serum albumin
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Shim Ha-Eun
Jeon Jong-Ho
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Abstract
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We demonstrate a detail protocol for the radiosynthesis of a 125I-labeled tetrazine prosthetic group and its application to the efficient radiolabeling of trans-cyclooctene-group conjugated human serum albumin (3) using inverse-electron-demand Diels-Alder reaction. Radioiodination of the stannylated precursor (2) was carried out by using [125I]NaI and chloramine T as an oxidant at room temperature for 15 min. After HPLC purification of the crude product, the purified 125I-labeled azide ([125I]1) was obtained with high radiochemical yield (65 ± 8%, n = 5) and excellent radiochemical purity (>99%). Inverse-electron-demand Diels-Alder reaction between ([125I]1) and 3 gave the 125I-labeled human serum albumin ([125I]4) with more than 99% of radiochemical yield as determined by radio-thin-layer chromatography (radio-TLC). These results clearly indicate that the present radiolabeling method will be useful for the efficient and convenient radiolabeling of trans-cyclooctene-group containing biomolecules.
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KEYWORD
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Radiolabeling, Radioactive iodine, Bioconjugation, Tetrazine, Albumin
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