Source:http://linkedlifedata.com/resource/pubmed/id/12552343
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
2
|
| pubmed:dateCreated |
2003-1-28
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| pubmed:abstractText |
Demobesin 1 is a potent new GRP-R-selective bombesin (BN) analogue containing an open chain tetraamine chelator for stable technetium-99m binding. Following a convenient labelling protocol, the radiopeptide, [(99m)Tc]Demobesin 1, formed in nearly quantitative yields and with high specific activities. Both unlabelled and labelled peptide demonstrated high-affinity binding in membrane preparations of the human androgen-independent prostate adenocarcinoma PC-3 cell line. The IC(50) values determined for Demobesin 1 and [Tyr(4)]BN were 0.70+/-0.08 n M and 1.5+/-0.20 n M, respectively, while the K(d) defined for [(99m)Tc/(99g)Tc]Demobesin 1 was 0.67+/-0.10 n M. [(99m)Tc]Demobesin 1 was rather stable in murine plasma, whereas it degraded rapidly in kidney and liver homogenates. After injection in healthy Swiss albino mice, [(99m)Tc]Demobesin 1 accumulated very efficiently in the target organs (pancreas, intestinal tract) via a GRP-R-mediated process, as shown by in vivo receptor blocking experiments. An equally high and GRP-R-mediated uptake was exhibited by [(99m)Tc]Demobesin 1 after injection in PC-3 tumour-bearing athymic mice. The initial high radioligand uptake of 16.2+/-3.1%ID/g in the PC-3 xenografts at 1 h p.i. remained at a similar level (15.61+/-1.19%ID/g) at 4 h p.i. Even after 24 h p.i., when the radioactivity had cleared from all other tissues, a value of 5.24+/-0.67%ID/g was still observed in the tumour. The high and prolonged localization of [(99m)Tc]Demobesin 1 at the tumour site and its rapid background clearance are very promising qualities for GRP-R-targeted tumour imaging in man.
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| pubmed:language |
eng
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| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Feb
|
| pubmed:issn |
1619-7070
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| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
30
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| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
247-58
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| pubmed:dateRevised |
2006-11-15
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| pubmed:meshHeading |
pubmed-meshheading:12552343-Animals,
pubmed-meshheading:12552343-Bombesin,
pubmed-meshheading:12552343-Cell Membrane,
pubmed-meshheading:12552343-Female,
pubmed-meshheading:12552343-Gastrin-Releasing Peptide,
pubmed-meshheading:12552343-Humans,
pubmed-meshheading:12552343-Isotope Labeling,
pubmed-meshheading:12552343-Kidney,
pubmed-meshheading:12552343-Liver,
pubmed-meshheading:12552343-Male,
pubmed-meshheading:12552343-Metabolic Clearance Rate,
pubmed-meshheading:12552343-Muscle, Skeletal,
pubmed-meshheading:12552343-Neoplasm Transplantation,
pubmed-meshheading:12552343-Organ Specificity,
pubmed-meshheading:12552343-Organotechnetium Compounds,
pubmed-meshheading:12552343-Prostatic Neoplasms,
pubmed-meshheading:12552343-Protein Binding,
pubmed-meshheading:12552343-Radiopharmaceuticals,
pubmed-meshheading:12552343-Tissue Distribution,
pubmed-meshheading:12552343-Tumor Cells, Cultured
|
| pubmed:year |
2003
|
| pubmed:articleTitle |
[99mTc]Demobesin 1, a novel potent bombesin analogue for GRP receptor-targeted tumour imaging.
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| pubmed:affiliation |
Institute of Radioisotopes--Radiodiagnostic Products, National Center for Scientific Research Demokritos, 15310 Ag. Paraskevi, Attikis, Athens, Greece.
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| pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't,
Evaluation Studies
|