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Efficient 125I-radiolabeling of biomolecules using a strain-promoted oxidation-controlled cyclooctyne-1,2-quinone
Sajid Mushtaq1, Sang Hyun Park
1Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, Jeonbuk 56212, Republic of Korea. parksh@kaeri.re.kr.
Abstract:
We report a novel 1,2-catechol based radioiodinated precursor for radioiodination of bicyclo[6.1.0]nonyne (BCN) installed biologically active molecules using a strain-promoted oxidation-controlled cyclooctyne-1,2-quinone cycloaddition reaction (SPOCQ) under ambient conditions. Compared to the reported methodologies, the new strategy demonstrates some clear advantages, including high in vitro and in vivo stability, high radiochemical yield, and exceptionally fast reaction kinetics at micro-molar concentration.
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