Activity of Hydrolytic Enzymes in Tumour Cells is a Determinant for Anti-tumour Efficacy of the Melphalan Containing Prodrug J1

@article{Gullbo2003ActivityOH,
  title={Activity of Hydrolytic Enzymes in Tumour Cells is a Determinant for Anti-tumour Efficacy of the Melphalan Containing Prodrug J1},
  author={J. Gullbo and M. Wickstr{\"o}m and Marcus Tullberg and H. Ehrsson and R. Lewensohn and P. Nygren and K. Luthman and R. Larsson},
  journal={Journal of Drug Targeting},
  year={2003},
  volume={11},
  pages={355 - 363}
}
Recently, we presented a series of melphalan containing di- and tripeptides with high cytotoxic activity and J1 (l-melphalanyl-p-l-fluorophenylalanine ethyl ester) was identified as one of the most interesting compounds. It was speculated that the increased activity compared to melphalan itself, demonstrated both in vitro and in vivo, resided in increased transport over the tumour cell membrane and/or hydrolytic cleavage and liberation of melphalan inside the cells. Indeed, overexpression of… Expand
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