Session
Speaker
The D-Enantiomer Of 2-131i-Phenylalanine As A New Promising
Theragnostic In Cancer
John J. Mertens, M. Bauwens, and L. Wiman
Belgium
Amino acid transporters do not only play an important role in nutrition
and neurology but also in cancer. A majority of cancer cells show
an over-expression of the LAT1 amino acid transport system. LAT1 has
the particularity to transport also D-enantiomers of phenylalanine.
We have proven that 131I-D-2-I-Phenylalanine is taken up in several
human cancer cell types like myeloma, glioma, astrocytoma, NSCLCarcinoma,
melanoma, pancreas carcinoma, colon adenocarcinoma, breast tumour
cells. The uptake in tumours in nude mice and human brain tumours
was high and the clearance from organs and background tissue was much
faster than of the L-enantiomer resulting in a higher tumour / tissue
or organ ratio. Moreover it was shown that in tumour bearing mice
the tumour growth could be inhibited by intravenous injection of 131I-D-2-I-Phenylalanine.
The fact that the D-phenylalanine analogues can cross the BBB, opens
a future for the radionuclidic therapy of brain tumours and brain
invading cancer cells not attainable by anti-body or peptide like
pharmaceuticals.
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