Article (Scientific journals)
New radioiodinated carboxylic and hydroxamic matrix metalloproteinase inhibitor tracers as potential tumor imaging agents
Oltenfreiter, Ruth; Staelens, Ludovicus; Lejeune, Annabelle et al.
2004In Nuclear Medicine and Biology, 31 (4), p. 459-468
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Keywords :
radiolabelled MMP inhibitors; iodine-123; in vitro assay; in vivo biodistribution; SPECT; tumor imaging
Abstract :
[en] Several studies have demonstrated a positive correlation between tumor progression and expression of extracellular proteinases such as matrix metalloproteinases (MMPs). MMP-2 and MMP-9 have become attractive targets for cancer research because of their increased expression in human malignant tumor tissues of various organs, providing a target for medical imaging techniques. Radioiodinated carboxylic and hydroxamic MMP inhibitors 2-(4'-[123]iodo-biphenyl-4-sulfonylainino)-3-(1H-indol-3-yl)-propionic acid (9) and 2-(4'-[I-123] iodo-biphenyl-4-sulfonylamino)-3-(1H-indol-3-yl)-propionamide (11) were synthesized by electrophilic aromatic substitution of the tributylstannyl derivatives and resulted in radiochemical yields of 60% +/- 5% (n - 3) and 70% +/- 5% (n = 6), respectively. In vitro zymography and enzyme assays showed high inhibition capacities of the inhibitors on gelatinases. In vivo biodistribution showed no long-terin accumulation in organs and the possibility to accumulate in the tumor. These results warrant further studies of radioiodinated carboxylic and hydroxamic MNIP inhibitor tracers as potential SPECT tumor imaging agents. (C) 2004 Elsevier Inc. All rights reserved.
Disciplines :
Radiology, nuclear medicine & imaging
Author, co-author :
Oltenfreiter, Ruth;  Ghent University
Staelens, Ludovicus;  Ghent University
Lejeune, Annabelle ;  Université de Liège - ULiège > Département des sciences de la vie > GIGA-R : Biologie et génétique moléculaire
Dumont, Filip
Frankenne, Francis 
Foidart, Jean-Michel ;  Université de Liège - ULiège > Département des sciences cliniques > Gynécologie - Obstétrique
Slegers, Guido
Language :
English
Title :
New radioiodinated carboxylic and hydroxamic matrix metalloproteinase inhibitor tracers as potential tumor imaging agents
Publication date :
May 2004
Journal title :
Nuclear Medicine and Biology
ISSN :
0969-8051
Publisher :
Pergamon Press, Oxford, United Kingdom
Volume :
31
Issue :
4
Pages :
459-468
Peer reviewed :
Peer Reviewed verified by ORBi
Available on ORBi :
since 07 April 2009

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