New Macrobicyclic Chelator for the Development of Ultrastable 64Cu-Radiolabeled Bioconjugate

被引：33

作者：

Pandya, Darpan N. ^{[1
]}

Dale, Ajit V. ^{[1
]}

Kim, Jung Young ^{[2
]}

Lee, Hochun ^{[3
]}

Ha, Yeong Su ^{[1
]}

An, Gwang Il ^{[2
]}

Yoo, Jeongsoo ^{[1
]}

机构：

[1] Kyungpook Natl Univ, Dept Mol Med, Taegu 700422, South Korea

[2] Korea Inst Radiol & Med Sci, Mol Imaging Res Ctr, Seoul 139706, South Korea

[3] Daegu Gyeongbuk Inst Sci & Technol, Dept Energy Syst Engn, Taegu 711873, South Korea

来源：

BIOCONJUGATE CHEMISTRY | 2012年 / 23卷 / 03期

关键词：

IN-VIVO BEHAVIOR; POSITRON-EMISSION-TOMOGRAPHY; SMALL-ANIMAL PET/CT; COPPER-64; RADIOPHARMACEUTICALS; TETRAAZAMACROCYCLIC COMPLEXES; BIFUNCTIONAL CHELATOR; BIOLOGICAL EVALUATION; PEPTIDE; CANCER; RADIONUCLIDES;

D O I：

10.1021/bc200539t

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

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

引用

页码：330 / 335

页数：6

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