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

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

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Received: 1 April 2013; in revised form: 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
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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.

AMA Style

Pellegrini PA, Howell NR, Shepherd RK, Lengkeek NA, Oehlke E, Katsifis AG, 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(6):7160-7178.

Chicago/Turabian Style

Pellegrini, Paul A.; Howell, Nicholas R.; Shepherd, Rachael K.; Lengkeek, Nigel A.; Oehlke, Elisabeth; Katsifis, Andrew G.; Greguric, Ivan. 2013. "Synthesis and Radiolabelling of DOTA-Linked Glutamine Analogues with 67,68Ga as Markers for Increased Glutamine Metabolism in Tumour Cells." Molecules 18, no. 6: 7160-7178.


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