7-Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase

被引：74

作者：

Balzarini, J

Gamboa, AE

Esnouf, R

Liekens, S

Neyts, J

De Clercq, E

Camarasa, MJ

Pérez-Pérez, MJ

机构：

[1] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium

[2] CSIC, Inst Quim Med, Madrid 28006, Spain

来源：

FEBS LETTERS | 1998年 / 438卷 / 1-2期

关键词：

thymidine phosphorylase; angiogenesis; 7-deazaxanthine; 6-amino-5-bromouracil; TPase inhibitor;

D O I：

10.1016/S0014-5793(98)01271-X

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

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 mu M in the presence of 100 mu M 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. (C) 1998 Federation of European Biochemical Societies.

引用

页码：91 / 95

页数：5

共 21 条

[1] PHOSPHOROLYSIS OF (E)-5-(2-BROMOVINYL)-2'-DEOXYURIDINE (BVDU) AND OTHER 5-SUBSTITUTED-2'-DEOXYURIDINES BY PURIFIED HUMAN THYMIDINE PHOSPHORYLASE AND INTACT BLOOD-PLATELETS [J].