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Molecules 2013, 18(6), 7160-7178; doi:10.3390/molecules18067160

Synthesis and Radiolabelling of DOTA-Linked Glutamine Analogues with 67,68Ga as Markers for Increased Glutamine Metabolism in Tumour Cells

Australian Nuclear Science and Technology Organisation, Locked Bag 2001 Kirrawee DC, NSW 2234, Australia
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Received: 1 April 2013 / Revised: 10 May 2013 / Accepted: 8 June 2013 / Published: 19 June 2013
(This article belongs to the Special Issue PET Chemistry in Molecular Imaging)
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Abstract

DOTA-linked glutamine analogues with a C6- alkyl and polyethyleneglycol (PEG) chain between the chelating group and the L-glutamine moiety were synthesised and labelled with 67,68Ga using established methods. High yields were achieved for the radiolabelling of the molecules with both radionuclides (>90%), although conversion of the commercially available 67Ga-citrate to the chloride species was a requirement for consistent high radiochemical yields. The generator produced 68Ga was in the [68Ga(OH)4] form. The 67Ga complexes and the 67Ga complexes were demonstrated to be stable in PBS buffer for a week. Uptake studies were performed with longer lived 67Ga analogues against four tumour cell lines, as well as uptake inhibition studies against L-glutamine, and two known amino acid transporter inhibitors. Marginal uptake was exhibited in the PEG variant radio-complex, and inhibition studies indicate this uptake is via a non-targeted amino acid pathway.
Keywords: PET; 67,68gallium; glutamine; amino acid transporter; radiochemistry; DOTA PET; 67,68gallium; glutamine; amino acid transporter; radiochemistry; DOTA
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MDPI and ACS Style

Pellegrini, P.A.; Howell, N.R.; Shepherd, R.K.; Lengkeek, N.A.; Oehlke, E.; Katsifis, A.G.; Greguric, I. Synthesis and Radiolabelling of DOTA-Linked Glutamine Analogues with 67,68Ga as Markers for Increased Glutamine Metabolism in Tumour Cells. Molecules 2013, 18, 7160-7178.

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