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KMID : 1145520180040020085
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Journal of Radiopharmaceuticals and Molecular Probes
2018 Volume.4 No. 2 p.85 ~ p.89
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Synthesis of 125I-labeled thiol-reactive prosthetic group for site-specific radiolabeling of human serum albumin
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Shim Ha-Eun
Song Lee
Jeon Jong-Ho
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Abstract
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We demonstrate a detail protocol for the radiosynthesis of an 125I-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 [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 MSTP ([125I]1) was obtained with high radiochemical yield (73 ± 5%, n = 3) and excellent radiochemical purity (>99%). Site-specific reaction between ([125I]1) and HSA gave the 125I-labeled human serum albumin ([125I]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.
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KEYWORD
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Radiolabeling, , Radioactive iodine, Site-specific reaction, MSTP, Human serum albumin
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