title: 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.
authors.affiliation: Department of Radiology, University of Pittsburgh, 100 Technology Drive, Suite 452F, Pittsburgh, PA 15219, USA. andersoncj@upmc.edu.
authors.forename: Dexing
authors.initials: D
authors.lastname: Zeng
authors.forename: Qin
authors.initials: Q
authors.lastname: Ouyang
authors.forename: Zhengxin
authors.initials: Z
authors.lastname: Cai
authors.forename: Xiang-Qun
authors.initials: XQ
authors.lastname: Xie
authors.forename: Carolyn J
authors.initials: CJ
authors.lastname: Anderson
mesh_terms: D053961:Azabicyclo Compounds / Q000097:blood / Q000138:chemical synthesis / Q000737:chemistry*; D002614:Chelating Agents / Q000138:chemical synthesis / Q000737:chemistry*; D003301:Copper Radioisotopes / Q000737:chemistry*; D004355:Drug Stability; D006571:Heterocyclic Compounds / Q000097:blood / Q000138:chemical synthesis / Q000737:chemistry*; D008958:Models, Molecular; D008968:Molecular Conformation; D063065:Organophosphonates / Q000097:blood / Q000138:chemical synthesis / Q000737:chemistry*
chemical_list: D053961:Azabicyclo Compounds; D002614:Chelating Agents; D003301:Copper Radioisotopes; D006571:Heterocyclic Compounds; D063065:Organophosphonates; C024560:cyclam