title: Propylene cross-bridged macrocyclic bifunctional chelator: a new design for facile bioconjugation and robust (64)Cu complex stability.
abstract: The first macrocyclic bifunctional chelator incorporating propylene cross-bridge was efficiently synthesized from cyclam in seven steps. After the introduction of an extra functional group for facile conjugation onto the propylene cross-bridge, the two carboxylic acid pendants could contribute to strong coordination of Cu(II) ions, leading to a robust Cu complex. The cyclic RGD peptide conjugate of PCB-TE2A-NCS was prepared and successfully radiolabeled with (64)Cu ion. The radiolabeled peptide conjugate was evaluated in vivo through a biodistribution study and animal PET imaging to demonstrate high tumor uptake with low background.
authors.affiliation: Department of Molecular Medicine, BK21 Plus KNU Biomedical Convergence Program, Kyungpook National University , Daegu 700-422, South Korea.
authors.forename: Darpan N
authors.initials: DN
authors.lastname: Pandya
authors.forename: Nikunj
authors.initials: N
authors.lastname: Bhatt
authors.forename: Gwang Il
authors.initials: GI
authors.lastname: An
authors.forename: Yeong Su
authors.initials: YS
authors.lastname: Ha
authors.forename: Nisarg
authors.initials: N
authors.lastname: Soni
authors.forename: Hochun
authors.initials: H
authors.lastname: Lee
authors.forename: Yong Jin
authors.initials: YJ
authors.lastname: Lee
authors.forename: Jung Young
authors.initials: JY
authors.lastname: Kim
authors.forename: Woonghee
authors.initials: W
authors.lastname: Lee
authors.forename: Heesu
authors.initials: H
authors.lastname: Ahn
authors.forename: Jeongsoo
authors.initials: J
authors.lastname: Yoo
mesh_terms: D000475:Alkenes / Q000737:chemistry*; D000818:Animals; D002614:Chelating Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D056831:Coordination Complexes / Q000737:chemistry; D003300:Copper / Q000737:chemistry*; D003301:Copper Radioisotopes / Q000737:chemistry / Q000493:pharmacokinetics; D015195:Drug Design; D005909:Glioblastoma / Q000378:metabolism / Q000473:pathology; D006571:Heterocyclic Compounds / Q000737:chemistry; D006801:Humans; D047028:Macrocyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry*; D051379:Mice; D008819:Mice, Nude; D008956:Models, Chemical; D015394:Molecular Structure; D009842:Oligopeptides / Q000737:chemistry; D049268:Positron-Emission Tomography / Q000379:methods; D051381:Rats; D014018:Tissue Distribution; D014183:Transplantation, Heterologous
chemical_list: D000475:Alkenes; D002614:Chelating Agents; D056831:Coordination Complexes; D003301:Copper Radioisotopes; D006571:Heterocyclic Compounds; D047028:Macrocyclic Compounds; D009842:Oligopeptides; C024560:cyclam; D003300:Copper; C047981:arginyl-glycyl-aspartic acid; C013658:propylene