7‐Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase

FEBS Letters

De Clercq, Erik¹  Gamboa, Antonio Esteban²  Liekens, Sandra¹  Neyts, Johan¹  Balzarini, Jan¹  Pérez-Pérez, Maria-Jesus²  Camarasa, Maria-José²  Esnouf, Robert¹ 

[1] Rega Institute for Medical Research, K.U. Leuven, Minderbroedersstraat 10, B-3000 Louvain, Belgium;Instituto de Quı́mica Médica, CSIC, 28006 Madrid, Spain

关键词: Thymidine phosphorylase;    Angiogenesis;    7-Deazaxanthine;    6-Amino-5-bromouracil;    TPase inhibitor;   

DOI  :  10.1016/S0014-5793(98)01271-X

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

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 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.

【 授权许可】

Unknown