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http://dx.doi.org/10.22643/JRMP.2018.4.2.85

Synthesis of ¹²⁵I-labeled thiol-reactive prosthetic group for site-specific radiolabeling of human serum albumin

Shim, Ha Eun (Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute)
Song, Lee (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.4, no.2, 2018 , pp. 85-89 More about this Journal

Abstract

We demonstrate a detail protocol for the radiosynthesis of an $^{125}I$ -labeled MSTP prosthetic group and its application to the efficient radiolabeling of human serum albumin (HSA). Radioiodination of the 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 MSTP ( $$[^{125}I$ $]$ $1$$ ) was obtained with high radiochemical yield ( $73{\pm}5%$ , n = 3) and excellent radiochemical purity (>99%). Site-specific reaction between ( $$[^{125}I$ $]$ $1$$ ) and HSA gave the $^{125}I$ -labeled human serum albumin ( $$[^{125}I$ $]$ $3$$ ) with more than 99% of radiochemical yield as determined by radio-thin-layer chromatography (radio-TLC). These results clearly demonstrate that the present radiolabeling method will be useful for the efficient and convenient radiolabeling of thiol-bearing biomolecules.

Keywords

Radiolabeling; Radioactive iodine; Site-specific reaction; MSTP; Human serum albumin;

Citations & Related Records

Reference

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KSCI

Synthesis of 125I-labeled thiol-reactive prosthetic group for site-specific radiolabeling of human serum albumin

Synthesis of ¹²⁵I-labeled thiol-reactive prosthetic group for site-specific radiolabeling of human serum albumin