title: Development of bifunctional chelates bearing hydroxamate arms for highly efficient (64)Cu radiolabeling.
abstract: Convenient approaches for the synthesis of DOTHA2 and NOTHA2, two cyclic bifunctional chelates (BFCs) bearing hydroxamate arms, have been developed. These novel BFCs coordinate (64)Cu with fast kinetics at room temperature in a wide range of concentrations and pH. The corresponding radiochemical complexes showed high stability, low residual activity in various tissues, and fast clearance in normal mice. The ability to conjugate DOTHA2 to both a small peptide and a large protein is also reported.
authors.affiliation: Department of Nuclear Medicine and Radiobiology, Université de Sherbrooke , 3001 12th North Avenue Sherbrooke, Quebec J1H 5N4, Canada.
authors.forename: Samia
authors.initials: S
authors.lastname: Ait-Mohand
authors.forename: Céline
authors.initials: C
authors.lastname: Denis
authors.forename: Geneviève
authors.initials: G
authors.lastname: Tremblay
authors.forename: Michel
authors.initials: M
authors.lastname: Paquette
authors.forename: Brigitte
authors.initials: B
authors.lastname: Guérin
mesh_terms: D000818:Animals; D002614:Chelating Agents / Q000138:chemical synthesis* / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D006877:Hydroxamic Acids / Q000737:chemistry*; D007700:Kinetics; D051379:Mice; D015394:Molecular Structure; D010455:Peptides / Q000737:chemistry*; D019275:Radiopharmaceuticals / Q000737:chemistry
chemical_list: D002614:Chelating Agents; D006877:Hydroxamic Acids; D010455:Peptides; D019275:Radiopharmaceuticals