Source:http://linkedlifedata.com/resource/pubmed/id/18341272
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
2008-4-16
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pubmed:abstractText |
Achieving high-yielding, robust, and reproducible chemistry is a prerequisite for the (18)F-labeling of peptides for quantitative receptor imaging using positron emission tomography (PET). In this study, we extend the toolbox of oxime chemistry to include the novel prosthetic groups [(18)F]-(2-{2-[2-(2-fluoroethoxy)ethoxy]ethoxy}ethoxy)acetaldehyde, [(18)F]5, and [(18)F]-4-(3-fluoropropoxy)benzaldehyde, [(18)F]9, in addition to the widely used 4-[(18)F]fluorobenzaldehyde, [(18)F]12. The three (18)F-aldehydes were conjugated to the same aminooxy-bearing RGD peptide and the effect of the prosthetic group on biodistribution and tumor uptake studied in mice. The peptide conjugate [(18)F]7 was found to possess superior in vivo pharmacokinetics with higher tumor to blood, tumor to liver, tumor to muscle, and tumor to lung ratios than either [(18)F]10 or [(18)F]13. The radioactivity from the [(18)F]7 conjugate excreted more extensively through the kidney route with 79%id passing through the urine and bladder at the 2 h time point compared to around 55%id for the more hydrophobic conjugates [(18)F]10 and [(18)F]13. The chemical nature of a prosthetic group can be employed to tailor the overall biodistribution profile of the radiotracer. In this example, the hydrophilic nature of the ethylene glycol containing prosthetic group [(18)F]5 clearly influences the overall excretion pattern for the RGD peptide conjugate.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Aldehydes,
http://linkedlifedata.com/resource/pubmed/chemical/Fluorine Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Integrins,
http://linkedlifedata.com/resource/pubmed/chemical/Peptides, Cyclic,
http://linkedlifedata.com/resource/pubmed/chemical/Polyethylene Glycols,
http://linkedlifedata.com/resource/pubmed/chemical/cyclic arginine-glycine-aspartic...
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
1520-4812
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
951-7
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:18341272-Aldehydes,
pubmed-meshheading:18341272-Animals,
pubmed-meshheading:18341272-Binding, Competitive,
pubmed-meshheading:18341272-Carcinoma, Lewis Lung,
pubmed-meshheading:18341272-Cell Line, Tumor,
pubmed-meshheading:18341272-Fluorine Radioisotopes,
pubmed-meshheading:18341272-Hydrophobic and Hydrophilic Interactions,
pubmed-meshheading:18341272-Integrins,
pubmed-meshheading:18341272-Mice,
pubmed-meshheading:18341272-Neovascularization, Pathologic,
pubmed-meshheading:18341272-Peptides, Cyclic,
pubmed-meshheading:18341272-Polyethylene Glycols,
pubmed-meshheading:18341272-Positron-Emission Tomography
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pubmed:year |
2008
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pubmed:articleTitle |
Radiosynthesis and biodistribution of cyclic RGD peptides conjugated with novel [18F]fluorinated aldehyde-containing prosthetic groups.
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pubmed:affiliation |
Hammersmith Imanet, Du Cane Road, London W12ONN, UK.
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pubmed:publicationType |
Journal Article
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