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7‐Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase
Author(s) -
Balzarini Jan,
Gamboa Antonio Esteban,
Esnouf Robert,
Liekens Sandra,
Neyts Johan,
De Clercq Erik,
Camarasa Maria-José,
Pérez-Pérez Maria-Jesus
Publication year - 1998
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/s0014-5793(98)01271-x
Subject(s) - thymidine phosphorylase , chorioallantoic membrane , thymidine , glycogen phosphorylase , thymine , chemistry , biochemistry , enzyme , ic50 , angiogenesis , biology , dna , in vitro , genetics
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 (IC 50 ) of 7DX was 40 μM in the presence of 100 μM 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.