The 2nd International Conference on Drug Discovery & Therapy: Dubai, February 1 - 4, 2010


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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