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Title: Synthesis and radiolabelling of DOTA-linked glutamine analogues with 67,68Ga as markers for increased glutamine metabolism in tumour cells
Authors: Pellegrini, PA
Howell, NR
Shepherd, RK
Lengkeek, NA
Oehlke, E
Katsifis, A
Greguric, I
Keywords: Tumor cells
Gallium 67
Gallium 68
Positron computed tomography
Polyethylene glycols
Amino acids
Issue Date: 19-Jun-2013
Publisher: MDPI (Multidisciplinary Digital Publishing Institute)
Citation: Pellegrini, P. A., Howell, N. R., Shepherd, R. K., Lengkeek, N. A., Oehlke, E., Katsifis, A. G., & Greguric, I. (2013). Synthesis and radiolabelling of DOTA-linked glutamine analogues with 67, 68Ga as markers for increased glutamine metabolism in tumour cells. Molecules, 18(6), 7160-7178. doi:10.3390/molecules18067160
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. © 2013 by the authors
Gov't Doc #: 8846
ISSN: 1420-3049
Appears in Collections:Journal Articles

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