title: A trithiolate tripodal bifunctional ligand for the radiolabeling of peptides with gallium(III).
abstract: A tripodal bifunctional chelator for gallium has been prepared with a chelation core consisting of three thiols and a tertiary amine. The synthesis proceeds in 13 steps with an overall yield of 22%. An aromatic amine is available for conjugation to peptides through carbodiimide coupling. Gallium(III) complexes were readily prepared from both the bifunctional chelator and a phenylalanine-conjugated system. These complexes underwent stability evaluation and were found to be stable to ligand exchange and enzymatic hydrolysis. This bifunctional chelator appears to be suitable for conjugation to peptides for the preparation of gallium radiopharmaceuticals.
authors.affiliation: Department of Chemistry, University of Illinois, Urbana, Illinois 61801, USA.
authors.forename: Leonard G
authors.initials: LG
authors.lastname: Luyt
authors.forename: John A
authors.initials: JA
authors.lastname: Katzenellenbogen
mesh_terms: D000588:Amines / Q000737:chemistry; D004355:Drug Stability; D005710:Gallium Radioisotopes / Q000737:chemistry*; D008024:Ligands; D015394:Molecular Structure; D010455:Peptides / Q000737:chemistry*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry; D013438:Sulfhydryl Compounds / Q000737:chemistry
chemical_list: D000588:Amines; D005710:Gallium Radioisotopes; D008024:Ligands; D010455:Peptides; D019275:Radiopharmaceuticals; D013438:Sulfhydryl Compounds