Synthesis and radiolabelling of DOTA-linked glutamine analogues with 67,68Ga as markers for increased glutamine metabolism in tumour cells

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dc.contributor.authorPellegrini, PAen_AU
dc.contributor.authorHowell, NRen_AU
dc.contributor.authorShepherd, Ren_AU
dc.contributor.authorLengkeek, NAen_AU
dc.contributor.authorOehlke, Een_AU
dc.contributor.authorKatsifis, Aen_AU
dc.contributor.authorGreguric, Ien_AU
dc.date.accessioned2020-03-23T06:28:55Zen_AU
dc.date.available2020-03-23T06:28:55Zen_AU
dc.date.issued2013-06-19en_AU
dc.description.abstractDOTA-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 authorsen_AU
dc.identifier.citationPellegrini, 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/molecules18067160en_AU
dc.identifier.govdoc8846en_AU
dc.identifier.issn1420-3049en_AU
dc.identifier.issue6en_AU
dc.identifier.journaltitleMoleculesen_AU
dc.identifier.pagination7160-7178en_AU
dc.identifier.urihttp://dx.doi.org/10.3390/molecules18067160en_AU
dc.identifier.urihttp://apo.ansto.gov.au/dspace/handle/10238/9193en_AU
dc.identifier.volume18en_AU
dc.language.isoenen_AU
dc.publisherMDPI (Multidisciplinary Digital Publishing Institute)en_AU
dc.subjectTumor cellsen_AU
dc.subjectGallium 67en_AU
dc.subjectGallium 68en_AU
dc.subjectGlutamineen_AU
dc.subjectRadiochemistryen_AU
dc.subjectPositron computed tomographyen_AU
dc.subjectPolyethylene glycolsen_AU
dc.subjectAmino acidsen_AU
dc.titleSynthesis and radiolabelling of DOTA-linked glutamine analogues with 67,68Ga as markers for increased glutamine metabolism in tumour cellsen_AU
dc.typeJournal Articleen_AU
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