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KMID : 1145520190050020083
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Journal of Radiopharmaceuticals and Molecular Probes
2019 Volume.5 No. 2 p.83 ~ p.88
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Facile radiolabeling of antibody-mimetic protein with In-111 via an inverse-electron-demand Diels- Alder reaction
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Nam You-Ree
Shim Ha-Eun
Lee Dong-Eun
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Abstract
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In order to understand the in vivo biodistribution of repebody protein (RB), an efficient and simple radiolabelingmethod for the protein is needed. We demonstrate a detailed protocol for the radiosynthesis of an 111Inradiolabeled tetrazine prosthetic group and its application to the efficient radiolabeling of trans-cyclooctenegroupconjugated repebody protein using inverse-electron-demand Diels-Alder reaction. First, 1,2,4,5-tetrazine(Tz) conjugated with a DOTA chelator, was used for preparing the radiolabeled DOTA complex with 111In.
Second, the trans-cyclooctene (TCO) functionalized repebody protein was synthesized which allows forthe preparation of radiolabeled proteins by copper-free click chemistry. Following incubation with the 111InradiolabeledDOTA complex (111In-Tz), the TCO-functionalized RB (TCO-RB) was radiolabeled successfullywith 111In, with a high radiochemical yield (69.5%) and radiochemical purity (>99%). The radiolabeling ofrepebody protein by copper-free click chemistry was accomplished within 20 min, with great efficiency inaqueous conditions. These results clearly indicate that the present radiolabeling method will be useful for theefficient and convenient radiolabeling of trans-cyclooctene-group containing biomolecules.
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KEYWORD
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Radiolabeling, In-111, invers-electron-demand Diels-Alder reaction, repebody protein, radio-ITLC
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