6533b7d4fe1ef96bd1263453

RESEARCH PRODUCT

[68Ga]Ga-DO2A-(OBu-l-tyr)2: Synthesis, 68Ga-radiolabeling and in vitro studies of a novel 68Ga-DO2A-tyrosine conjugate as potential tumor tracer for PET

Frederic ZollerFrank RoeschSimone MaschauerPatrick J. RissTorsten KuwertOlaf PranteCarsten Burchardt

subject

StereochemistryClinical BiochemistryPharmaceutical ScienceBiochemistryChemical synthesisCell Line TumorDrug DiscoveryOrganometallic CompoundsAnimalsChelationAmino acid transporterTyrosineMolecular BiologyGallium IsotopesFluoroethylBrain NeoplasmsChemistryOrganic ChemistryLigand (biochemistry)In vitroRatsPositron-Emission TomographyMolecular MedicineRadiopharmaceuticalsGlioblastomaConjugate

description

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.

yearjournalcountryeditionlanguage
2009-07-01Bioorganic & Medicinal Chemistry Letters
https://doi.org/10.1016/j.bmcl.2009.05.001