期刊论文详细信息
Molecules
Synthesis and Radiolabelling of DOTA-Linked Glutamine Analogues with 67,68Ga as Markers for Increased Glutamine Metabolism in Tumour Cells
Paul A. Pellegrini1  Nicholas R. Howell2  Rachael K. Shepherd2  Nigel A. Lengkeek2  Elisabeth Oehlke2  Andrew G. Katsifis2 
[1] id="af1-molecules-18-07160">Australian Nuclear Science and Technology Organisation, Locked Bag 2001 Kirrawee DC, NSW 2234, Austral
关键词: PET;    67;    68gallium;    glutamine;    amino acid transporter;    radiochemistry;    DOTA;   
DOI  :  10.3390/molecules18067160
来源: mdpi
PDF
【 摘 要 】

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.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.

【 预 览 】
附件列表
Files Size Format View
RO202003190035275ZK.pdf 510KB PDF download
  文献评价指标  
  下载次数:10次 浏览次数:14次