| pubmed-article:15828816 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:15828816 | lifeskim:mentions | umls-concept:C0027651 | lld:lifeskim |
| pubmed-article:15828816 | lifeskim:mentions | umls-concept:C0178539 | lld:lifeskim |
| pubmed-article:15828816 | lifeskim:mentions | umls-concept:C1280500 | lld:lifeskim |
| pubmed-article:15828816 | lifeskim:mentions | umls-concept:C0242209 | lld:lifeskim |
| pubmed-article:15828816 | lifeskim:mentions | umls-concept:C1160466 | lld:lifeskim |
| pubmed-article:15828816 | lifeskim:mentions | umls-concept:C0023688 | lld:lifeskim |
| pubmed-article:15828816 | lifeskim:mentions | umls-concept:C0599896 | lld:lifeskim |
| pubmed-article:15828816 | lifeskim:mentions | umls-concept:C0678640 | lld:lifeskim |
| pubmed-article:15828816 | lifeskim:mentions | umls-concept:C1533691 | lld:lifeskim |
| pubmed-article:15828816 | lifeskim:mentions | umls-concept:C1515655 | lld:lifeskim |
| pubmed-article:15828816 | lifeskim:mentions | umls-concept:C1707271 | lld:lifeskim |
| pubmed-article:15828816 | pubmed:issue | 8 | lld:pubmed |
| pubmed-article:15828816 | pubmed:dateCreated | 2005-4-14 | lld:pubmed |
| pubmed-article:15828816 | pubmed:abstractText | For effective targeting of somatostatin receptor (sst) expressing tumors by radiolabeled octreotide analogues, high ligand uptake into sst-positive cells is mandatory. To optimize it, two modifications have been introduced into [(125)I]Tyr(3)-octreotide ([(125)I]TOC): C-terminal Thr-for-Thr(ol) exchange (leading to Tyr(3)-octreotate (TOCA)) and N-terminal derivatization with different carbohydrates. Both have significant impact on radioligand uptake into sst(2)-expressing cells in vitro and in vivo. Glucose conjugation via Amadori reaction by itself led to improved tumor uptake of [(123)I]Gluc-TOC in vivo, which is based on an enhancement of peptide internalization despite a reduction in receptor affinity. In the case of the doubly modified analogues [(123)I]Gluc-TOCA, [(123)I]Gluc-S-TOCA, and [(123)I]Gal-S-TOCA, a cumulative effect of both structural modifications was observed, leading up to a 5-fold increased uptake of these compounds in sst-expressing tumors compared to [(125)I]TOC. Thus, glycosylation with small carbohydrates was found to be a suitable tool to enhance receptor-mediated uptake of radiolabeled octreotide analogues into sst-positive malignancies, leading to tracers with excellent characteristics for in vivo sst-imaging applications. | lld:pubmed |
| pubmed-article:15828816 | pubmed:language | eng | lld:pubmed |
| pubmed-article:15828816 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15828816 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:15828816 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15828816 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15828816 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15828816 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15828816 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15828816 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15828816 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15828816 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15828816 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15828816 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15828816 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:15828816 | pubmed:month | Apr | lld:pubmed |
| pubmed-article:15828816 | pubmed:issn | 0022-2623 | lld:pubmed |
| pubmed-article:15828816 | pubmed:author | pubmed-author:ReubiJean... | lld:pubmed |
| pubmed-article:15828816 | pubmed:author | pubmed-author:SchwaigerMark... | lld:pubmed |
| pubmed-article:15828816 | pubmed:author | pubmed-author:WesterHans-Jü... | lld:pubmed |
| pubmed-article:15828816 | pubmed:author | pubmed-author:SchotteliusMa... | lld:pubmed |
| pubmed-article:15828816 | pubmed:author | pubmed-author:EltschingerVe... | lld:pubmed |
| pubmed-article:15828816 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:15828816 | pubmed:day | 21 | lld:pubmed |
| pubmed-article:15828816 | pubmed:volume | 48 | lld:pubmed |
| pubmed-article:15828816 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:15828816 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:15828816 | pubmed:pagination | 2778-89 | lld:pubmed |
| pubmed-article:15828816 | pubmed:dateRevised | 2005-11-17 | lld:pubmed |
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| pubmed-article:15828816 | pubmed:year | 2005 | lld:pubmed |
| pubmed-article:15828816 | pubmed:articleTitle | N-terminal sugar conjugation and C-terminal Thr-for-Thr(ol) exchange in radioiodinated Tyr3-octreotide: effect on cellular ligand trafficking in vitro and tumor accumulation in vivo. | lld:pubmed |
| pubmed-article:15828816 | pubmed:affiliation | Nuklearmedizinische Klinik und Poliklinik, Klinikum rechts der Isar, Technische Universität München, 81675 München, Germany. M.Schottelius@lrz.tum.de | lld:pubmed |
| pubmed-article:15828816 | pubmed:publicationType | Journal Article | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:15828816 | lld:chembl |
