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New cross-bridged cyclam derivative CB-TE1K1P, an improved bifunctional chelator for copper radionuclides.

ABSTRACT: A new cross-bridged cyclam chelator, CB-TE1K1P, was developed for copper-based radiopharmaceuticals, and this chelator can be labelled with (64)Cu under mild conditions in high specific activity. DBCO-PEG4-CB-TE1K1P was synthesized for conjugation to proteins, while Dde-CB-TE1K1P((t)Bu2)-OH was synthesized for solid-phase peptide synthesis. Examples of the conjugation chemistry, radiolabelling and serum stability of each are presented.

SUBMITTER: Zeng D

PROVIDER: S-EPMC4277816 | biostudies-literature | 2014 Jan

REPOSITORIES: biostudies-literature

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New cross-bridged cyclam derivative CB-TE1K1P, an improved bifunctional chelator for copper radionuclides.

Zeng Dexing D Ouyang Qin Q Cai Zhengxin Z Xie Xiang-Qun XQ Anderson Carolyn J CJ

Chemical communications (Cambridge, England) 20140101 1

A new cross-bridged cyclam chelator, CB-TE1K1P, was developed for copper-based radiopharmaceuticals, and this chelator can be labelled with (64)Cu under mild conditions in high specific activity. DBCO-PEG4-CB-TE1K1P was synthesized for conjugation to proteins, while Dde-CB-TE1K1P((t)Bu2)-OH was synthesized for solid-phase peptide synthesis. Examples of the conjugation chemistry, radiolabelling and serum stability of each are presented. ...[more]

PMID: 24141371

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