7-Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase

  • FEBS Lett. 1998 Oct 30;438(1-2):91-5. doi: 10.1016/s0014-5793(98)01271-x.
J Balzarini  1 ,  A E Gamboa ,  R Esnouf ,  S Liekens ,  J Neyts ,  E De Clercq ,  M J Camarasa ,  M J Pérez-Pérez
Affiliations
  • 1. Rega Institute for Medical Research, K.U. Leuven, Louvain, Belgium.
PMID: 9821965 DOI: 10.1016/s0014-5793(98)01271-x
Abstract

7-Deazaxanthine (7DX) was identified as a novel inhibitor of thymidine (dThd) Phosphorylase (TPase). It inhibited the TPase reaction in a concentration-dependent manner. At 1 mM, it almost completely prevented the TPase-catalysed hydrolysis of dThd to thymine. The 50% inhibitory concentration (IC50 of 7DX was 40 microM in the presence of 100 microM of the natural substrate dThd. 7DX is also endowed with a marked inhibitory effect on angiogenesis. It significantly prevents neovascularisation in the chicken chorioallantoic membrane during development. 7DX is the first purine derivative shown to be a potent inhibitor of purified TPase and angiogenesis.

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