Next Article in Journal
Immunomodulatory Effect of Stichopus japonicus Acid Mucopolysaccharide on Experimental Hepatocellular Carcinoma in Rats
Next Article in Special Issue
A Fully Automated Radiosynthesis of [18F]Fluoroethyl-Diprenorphine on a Single Module by Use of SPE Cartridges for Preparation of High Quality 2-[18F]Fluoroethyl Tosylate
Previous Article in Journal
Applications of Azide-Based Bioorthogonal Click Chemistry in Glycobiology
Previous Article in Special Issue
89Zr, a Radiometal Nuclide with High Potential for Molecular Imaging with PET: Chemistry, Applications and Remaining Challenges
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

* , , , , ,  and
Australian Nuclear Science and Technology Organisation, Locked Bag 2001 Kirrawee DC, NSW 2234, Australia
* Author to whom correspondence should be addressed.
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)
Download PDF [511 KB, uploaded 18 June 2014]

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.

Share & Cite This Article

Further Mendeley | CiteULike
Export to BibTeX |
EndNote
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.

View more citation formats

Related Articles

Article Metrics

For more information on the journal, click here

Comments

Cited By

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert