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http://dx.doi.org/10.22643/JRMP.2017.3.2.98

Synthesis of ¹²⁵I-labeled tetrazine for efficient radiolabeling of human serum albumin

Shim, Ha Eun (Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute)
Jeon, Jongho (Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute)

Publication Information

Journal of Radiopharmaceuticals and Molecular Probes / v.3, no.2, 2017 , pp. 98-102 More about this Journal

Abstract

We demonstrate a detail protocol for the radiosynthesis of a $^{125}I-labeled$ 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 [ $^{125}I$ ]NaI and chloramine T as an oxidant at room temperature for 15 min. After HPLC purification of the crude product, the purified $^{125}I-labeled$ azide ([ $^{125}I$ ]1) was obtained with high radiochemical yield ( $65{\pm}8%$ , n = 5) and excellent radiochemical purity (>99%). Inverse-electron-demand Diels-Alder reaction between ([ $^{125}I$ ]1) and 3 gave the $^{125}I-labeled$ human serum albumin ([ $^{125}I$ ]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.

Keywords

Radiolabeling; Radioactive iodine; Bioconjugation; Tetrazine; Albumin;

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Times Cited By KSCI : 1 (Citation Analysis)

Reference
Cited By KSCI

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KSCI

Synthesis of 125I-labeled tetrazine for efficient radiolabeling of human serum albumin

Synthesis of ¹²⁵I-labeled tetrazine for efficient radiolabeling of human serum albumin