| pubmed-article:12552343 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:12552343 | lifeskim:mentions | umls-concept:C0027651 | lld:lifeskim |
| pubmed-article:12552343 | lifeskim:mentions | umls-concept:C0011923 | lld:lifeskim |
| pubmed-article:12552343 | lifeskim:mentions | umls-concept:C0005919 | lld:lifeskim |
| pubmed-article:12552343 | lifeskim:mentions | umls-concept:C0061132 | lld:lifeskim |
| pubmed-article:12552343 | lifeskim:mentions | umls-concept:C1333714 | lld:lifeskim |
| pubmed-article:12552343 | lifeskim:mentions | umls-concept:C0243071 | lld:lifeskim |
| pubmed-article:12552343 | lifeskim:mentions | umls-concept:C0679622 | lld:lifeskim |
| pubmed-article:12552343 | lifeskim:mentions | umls-concept:C0205314 | lld:lifeskim |
| pubmed-article:12552343 | pubmed:issue | 2 | lld:pubmed |
| pubmed-article:12552343 | pubmed:dateCreated | 2003-1-28 | lld:pubmed |
| pubmed-article:12552343 | 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. | lld:pubmed |
| pubmed-article:12552343 | pubmed:language | eng | lld:pubmed |
| pubmed-article:12552343 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12552343 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:12552343 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12552343 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12552343 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12552343 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12552343 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:12552343 | pubmed:month | Feb | lld:pubmed |
| pubmed-article:12552343 | pubmed:issn | 1619-7070 | lld:pubmed |
| pubmed-article:12552343 | pubmed:author | pubmed-author:ReubiJean... | lld:pubmed |
| pubmed-article:12552343 | pubmed:author | pubmed-author:MainaTheodosi... | lld:pubmed |
| pubmed-article:12552343 | pubmed:author | pubmed-author:NockBertholdB | lld:pubmed |
| pubmed-article:12552343 | pubmed:author | pubmed-author:NikolopoulouA... | lld:pubmed |
| pubmed-article:12552343 | pubmed:author | pubmed-author:LoudosGeorgeG | lld:pubmed |
| pubmed-article:12552343 | pubmed:author | pubmed-author:MaintasDimitr... | lld:pubmed |
| pubmed-article:12552343 | pubmed:author | pubmed-author:ChiotellisEfs... | lld:pubmed |
| pubmed-article:12552343 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:12552343 | pubmed:volume | 30 | lld:pubmed |
| pubmed-article:12552343 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:12552343 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:12552343 | pubmed:pagination | 247-58 | lld:pubmed |
| pubmed-article:12552343 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
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| pubmed-article:12552343 | pubmed:meshHeading | pubmed-meshheading:12552343... | lld:pubmed |
| pubmed-article:12552343 | pubmed:year | 2003 | lld:pubmed |
| pubmed-article:12552343 | pubmed:articleTitle | [99mTc]Demobesin 1, a novel potent bombesin analogue for GRP receptor-targeted tumour imaging. | lld:pubmed |
| pubmed-article:12552343 | pubmed:affiliation | Institute of Radioisotopes--Radiodiagnostic Products, National Center for Scientific Research Demokritos, 15310 Ag. Paraskevi, Attikis, Athens, Greece. | lld:pubmed |
| pubmed-article:12552343 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:12552343 | pubmed:publicationType | Comparative Study | lld:pubmed |
| pubmed-article:12552343 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| pubmed-article:12552343 | pubmed:publicationType | Evaluation Studies | lld:pubmed |
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