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Dokumenttyp:
journal article 
Autor(en):
Schottelius, M; Reubi, JC; Eltschinger, V; Schwaiger, M; Wester, HJ 
Titel:
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. 
Abstract:
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 v...    »
 
Zeitschriftentitel:
J Med Chem 
Jahr:
2005 
Band / Volume:
48 
Heft / Issue:
Seitenangaben Beitrag:
2778-89 
Sprache:
eng 
Print-ISSN:
0022-2623 
TUM Einrichtung:
Nuklearmedizinische Klinik und Poliklinik