FEBS Letters | |
7‐Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase | |
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
【 预 览 】
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