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New Macrobicyclic Chelator for the Development of Ultrastable Cu-64-Radiolabeled Bioconjugate
- New Macrobicyclic Chelator for the Development of Ultrastable Cu-64-Radiolabeled Bioconjugate
- Pandya, DN[Pandya, Darpan N.]; Dale, AV[Dale, Ajit V.]; Kim, JY[Kim, Jung Young]; Lee, H[Lee, Hochun]; Ha, YS[Ha, Yeong Su]; An, GI[An, Gwang Il]; Yoo, J[Yoo, Jeongsoo]
- DGIST Authors
- Lee, H[Lee, Hochun]
- Issue Date
- Bioconjugate Chemistry, 23(3), 330-335
- Article Type
- Acetic Acid; Animals; Bridged Compound; Chelating Agent; Chelating Agents; Chemical Reaction Kinetics; Chromatography, High Pressure Liquid; Complex Formation; Conjugate; Copper 64; Copper Complex; Copper Radioisotopes; Cyclam Derivative; Ethylene; Isotope Labeling; Macrocyclic Compound; Macrocyclic Compounds; Molecular Stability; Propylene; Quantitative Analysis; Rats; Rats, Sprague-Dawley; Reduction; Spectrophotometry, Ultraviolet; Synthesis
- Ethylene cross-bridged cyclam with two acetate pendant arms, ECB-TE2A, is known to form the most kinetically stable 64Cu complexes. However, its usefulness as a bifunctional chelator is limited because of its harsh radiolabeling conditions. Herein, we report new cross-bridged cyclam chelator for the development of ultrastable 64Cu-radiolabeled bioconjugates. Propylene cross-bridged TE2A (PCB-TE2A) was successfully synthesized in an efficient way. The Cu(II) complex of PCB-TE2A exhibited much higher kinetic stability than ECB-TE2A in acid decomplexation studies, and also showed high resistance to reduction-mediated demetalation. Furthermore, the quantitative radiolabeling of PCB-TE2A with 64Cu was achieved under milder conditions compared to ECB-TE2A. Biodistribution studies strongly indicate that the 64Cu complexes of PCB-TE2A cleared out rapidly from the body with minimum decomplexation. © 2012 American Chemical Society.
- American Chemical Society
- Related Researcher
Electrochemistry Laboratory for Sustainable Energy(ELSE)
Lithium-ion batteries; Novel Materials for rechargeable batteries; Novel energy conversion;storage systems; Electrochemistry; 리튬이차전지; 이차전지용 신규 전극 및 전해액; 신규 에너지변환 및 저장 시스템; 전기화학
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- Department of Energy Science and EngineeringElectrochemistry Laboratory for Sustainable Energy(ELSE)1. Journal Articles
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