| [18F]fluoromethyl-[1,2-2H4]-choline: a novel radiotracer for imaging choline metabolism in tumors by positron emission tomography. | |
| | |
MedLine Citation:
|
PMID: 19773436 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
Current radiotracers for positron emission tomography imaging of choline metabolism have poor systemic metabolic stability in vivo. We describe a novel radiotracer, [(18)F]fluoromethyl-[1,2-(2)H(4)]-choline (D4-FCH), that employs deuterium isotope effect to improve metabolic stability. D4-FCH proved more resistant to oxidation than its nondeuterated analogue, [(18)F]fluoromethylcholine, in plasma, kidneys, liver, and tumor, while retaining phosphorylation potential. Tumor radiotracer levels, a determinant of sensitivity in imaging studies, were improved by deuterium substitution; tumor uptake values expressed as percent injected dose per voxel at 60 min were 7.43 +/- 0.47 and 5.50 +/- 0.49 for D4-FCH and [(18)F]fluoromethylcholine, respectively (P = 0.04). D4-FCH was also found to be a useful response biomarker. Treatment with the mitogenic extracellular kinase inhibitor PD0325901 resulted in a reduction in tumor radiotracer uptake that occurred in parallel with reductions in choline kinase A expression. In conclusion, D4-FCH is a very promising metabolically stable radiotracer for imaging choline metabolism in tumors. |
| | |
Authors:
|
Julius Leyton; Graham Smith; Yongjun Zhao; Meg Perumal; Quang-De Nguyen; Edward Robins; Erik Arstad; Eric O Aboagye |
Related Documents
:
|
8074956 - Fdg-pet for the evaluation of tumor viability after anticancer therapy. 19445476 - Tumor imaging and therapy using radiolabeled somatostatin analogues. 9255146 - Breast imaging with fluorine-18-fdg pet: quantitative image analysis. 20863096 - A reexamination of active and passive tumor targeting by using rod-shaped gold nanocrys... 2584706 - Contribution of il-6 to the antiproliferative effect of il-1 and tumor necrosis factor ... 16436596 - Loss of p53 induces changes in the behavior of subventricular zone cells: implication f... |
Publication Detail:
|
Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2009-09-22 |
Journal Detail:
|
Title: Cancer research Volume: 69 ISSN: 1538-7445 ISO Abbreviation: Cancer Res. Publication Date: 2009 Oct |
Date Detail:
|
Created Date: 2009-10-02 Completed Date: 2009-12-03 Revised Date: 2013-03-27 |
Medline Journal Info:
|
Nlm Unique ID: 2984705R Medline TA: Cancer Res Country: United States |
Other Details:
|
Languages: eng Pagination: 7721-8 Citation Subset: IM |
Affiliation:
|
Molecular Therapy Group, Faculty of Medicine, Imperial College London, London, United Kingdom. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Animals Benzamides / pharmacology Choline / analogs & derivatives*, diagnostic use, metabolism*, pharmacokinetics Colonic Neoplasms / metabolism, radionuclide imaging* Deuterium / diagnostic use*, pharmacokinetics Diphenylamine / analogs & derivatives, pharmacology HCT116 Cells Humans Melanoma / metabolism, radionuclide imaging* Mice Mice, Inbred BALB C Mice, Nude Oxidation-Reduction Positron-Emission Tomography / methods Radiopharmaceuticals / diagnostic use*, pharmacokinetics Tissue Distribution Transplantation, Heterologous |
| Grant Support | |
ID/Acronym/Agency:
|
A10337//Cancer Research UK; U1200.005.00001.01//Medical Research Council; //Cancer Research UK |
| Chemical | |
Reg. No./Substance:
|
0/Benzamides; 0/PD 0325901; 0/Radiopharmaceuticals; 0/fluoromethylcholine; 122-39-4/Diphenylamine; 62-49-7/Choline; 7782-39-0/Deuterium |
| Comments/Corrections | |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Rearrangements and amplification of IER3 (IEX-1) represent a novel and recurrent molecular abnormali...
Next Document: Expression of IFN-beta enhances both efficacy and safety of oncolytic vesicular stomatitis virus for...