title: [(68)Ga]Ga-DO(2)A-(OBu-l-tyr)(2): synthesis, (68)Ga-radiolabeling and in vitro studies of a novel (68)Ga-DO(2)A-tyrosine conjugate as potential tumor tracer for PET.
abstract: The synthesis, (68)Ga-labeling and in vitro study of the novel tyrosine chelate derivative [(68)Ga]Ga-1,4,7,10-tetraazacyclododecane-1,7-diacetic acid-4,10-di-(O-butyl)-l-tyrosine ([(68)Ga]Ga-DO(2)A-(OBu-l-tyr)(2)) as a potential tracer for imaging tumor metabolism by positron emission tomography (PET) is presented. This approach combines the biological amino acid transporter targeting properties of l-tyrosine with the outstanding availability of (68)Ga(III) via the (68)Ge/(68)Ga generator. In vitro studies utilizing the F98-glioblastoma cell line revealed specific uptake of [(68)Ga]Ga-DO2A-(OBu-l-tyr)(2) that was comparable to that of the reference O-(2-[(18)F]fluoroethyl)-l-tyrosine (FET). These promising results indicate a high potential of [(68)Ga]Ga-DO(2)A-(OBu-l-tyr)(2) for molecular imaging of tumor-driven amino acid uptake by PET.
authors.affiliation: Johannes Gutenberg-University Mainz, Institute of Nuclear Chemistry, Fritz-Strassmann-Weg 2, 55128 Mainz, Germany.
authors.forename: Carsten
authors.initials: C
authors.lastname: Burchardt
authors.forename: Patrick J
authors.initials: PJ
authors.lastname: Riss
authors.forename: Frederic
authors.initials: F
authors.lastname: Zoller
authors.forename: Simone
authors.initials: S
authors.lastname: Maschauer
authors.forename: Olaf
authors.initials: O
authors.lastname: Prante
authors.forename: Torsten
authors.initials: T
authors.lastname: Kuwert
authors.forename: Frank
authors.initials: F
authors.lastname: Roesch
mesh_terms: D000818:Animals; D001932:Brain Neoplasms / Q000175:diagnosis; D045744:Cell Line, Tumor; D005709:Gallium Isotopes / Q000737:chemistry; D005909:Glioblastoma / Q000175:diagnosis; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats
chemical_list: D005709:Gallium Isotopes; D009942:Organometallic Compounds; D019275:Radiopharmaceuticals