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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, ÀüÁ¾È£,
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 ( Shim Ha-Eun ) 
Korea Atomic Energy Research Institute Advanced Radiation Technology Institute

 ( Song Lee ) 
Korea Atomic Energy Research Institute Advanced Radiation Technology Institute
ÀüÁ¾È£ ( Jeon Jong-Ho ) 
Korea Atomic Energy Research Institute Advanced Radiation Technology Institute

Abstract


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 ¡¾ 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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Radiolabeling;, Radioactive iodine; Site-specific reaction; MSTP; Human serum albumin

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