Balzarini J, Gamboa A E, Esnouf R, Liekens S, Neyts J, De Clercq E, Camarasa M J, Pérez-Pérez M J
Rega Institute for Medical Research, K.U. Leuven, Louvain, Belgium.
FEBS Lett. 1998 Oct 30;438(1-2):91-5. doi: 10.1016/s0014-5793(98)01271-x.
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.
7-脱氮黄嘌呤（7DX）被鉴定为胸苷（dThd）磷酸化酶（TPase）的新型抑制剂。它以浓度依赖的方式抑制TPase反应。在1 mM时，它几乎完全阻止了TPase催化的dThd水解为胸腺嘧啶。在存在100 microM天然底物dThd的情况下，7DX的50%抑制浓度（IC50）为40 microM。7DX对血管生成也具有显著的抑制作用。它能显著阻止鸡胚绒毛尿囊膜发育过程中的新血管形成。7DX是首个被证明是纯化TPase和血管生成的有效抑制剂的嘌呤衍生物。
