New macrobicyclic chelator for the development of ultrastable 64Cu-radiolabeled bioconjugate

Bioconjugate Chemistry
Darpan N PandyaJeongsoo Yoo

Abstract

Ethylene cross-bridged cyclam with two acetate pendant arms, ECB-TE2A, is known to form the most kinetically stable (64)Cu 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 (64)Cu-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 (64)Cu was achieved under milder conditions compared to ECB-TE2A. Biodistribution studies strongly indicate that the (64)Cu complexes of PCB-TE2A cleared out rapidly from the body with minimum decomplexation.

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Citations

Jun 2, 2012·Inorganic Chemistry·Luís M P LimaRaphaël Tripier
Jul 26, 2013·Bioconjugate Chemistry·Darpan N PandyaJeongsoo Yoo
Jun 6, 2014·ACS Medicinal Chemistry Letters·Ajit V DaleJeongsoo Yoo
Dec 4, 2013·Molecular Pharmaceutics·Eszter BorosPeter Caravan
Feb 13, 2016·Dalton Transactions : an International Journal of Inorganic Chemistry·Thomas W PriceGraeme J Stasiuk
Oct 22, 2013·Chemical Communications : Chem Comm·Dexing ZengCarolyn J Anderson
Dec 19, 2013·Journal of Labelled Compounds & Radiopharmaceuticals·Zhengxin Cai, Carolyn J Anderson
Feb 8, 2021·Nuclear Medicine and Biology·Cathryn Helena Stanford DriverRoger Hunter

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