Reference : Synthesis, quality control and in vivo evaluation of [I-123] rhTIMP-2, a potential tu...
Scientific journals : Article
Human health sciences : Pharmacy, pharmacology & toxicology
Physical, chemical, mathematical & earth Sciences : Chemistry
Life sciences : Biochemistry, biophysics & molecular biology
Synthesis, quality control and in vivo evaluation of [I-123] rhTIMP-2, a potential tumour-imaging agent
Oltenfreiter, R. [> > > >]
Burvenich, I. [> > > >]
Staelens, L. [> > > >]
Lejeune, Annabelle [Université de Liège - ULiège > Département des sciences de la vie > GIGA-R : Biologie et génétique moléculaire >]
Frankenne, F. [> >]
Foidart, Jean-Michel mailto [Université de Liège - ULiège > Département des sciences cliniques > Gynécologie - Obstétrique >]
Slegers, G. [> > > >]
Journal of Labelled Compounds & Radiopharmaceuticals
John Wiley & Sons Ltd
[en] radiolabelled rhTIMP-2 ; iodine-123 ; in vivo biodistribution ; SPECT ; tumour imaging
[en] Matrix metalloproteinases (MMPs) are enzymes involved in the turnover of the extracellular matrix. Their overexpression in tumours may provide a target for diagnostic imaging by using labelled MMP inhibitors. MMPs are inhibited by endogenous tissue inhibitors of metalloproteinases (TIMPs). The enhanced production of MT1-MMP, located on the surface of cells within or in the direct vicinity of the tumour, and the high affinity interaction between TIMP-2 and MT1-MMP suggested that TIMP-2 could be a potential agent for non-invasive monitoring of cancer MMP levels, diagnosis of primary and secondary tumours and tumour response to MMP inhibitor therapy. There is also evidence that I-125-rhTIMP-2 internalizes, which is an important feature for its possible use as a radiotherapeuticum if labelled with I-131. Labelling of rhTIMP-2 was performed using the iodogen method resulting in a radiochemical yield of 51.1 +/- 11.8% (n = 5) and a radiochemical purity of > 98%. The trichloroacetic acid (TCA) precipitability of I-123 rhTIMP-2 was 95.2%. SDS-PAGE confirmed the correct size (21 kDa) of the purified I-123 rhTIMP-2 without degradation. HPLC showed one radioactive peak with a retention time corresponding to the nonlabelled rhTIMP-2. In vivo biodistribution showed no long-term accumulation in organs and the possibility to accumulate in the tumour. These results show the potential of I-123 rhTIMP-2 as tumour-imaging agent. Copyright (c) 2005 John Wiley

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