RATIONAL DESIGN FOR CYTOSOLIC DELIVERY OF NUCLEOSIDE MONOPHOSPHATES - SATE AND DTE AS ENZYME-LABILE TRANSIENT PHOSPHATE PROTECTING GROUPS

被引:111
作者
PERIGAUD, C [1 ]
GOSSELIN, G [1 ]
LEFEBVRE, I [1 ]
GIRARDET, JL [1 ]
BENZARIA, S [1 ]
BARBER, I [1 ]
IMBACH, JL [1 ]
机构
[1] UNIV MONTPELLIER 2, CHIM BIOORGAN LAB,CNRS,URA 488,CASE COURRIER 008, PL EUGENE BATAILLON, F-34095 MONTPELLIER 5, FRANCE
关键词
D O I
10.1016/S0960-894X(01)80709-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
It was demonstrated that the use of neutral 2',3'-dideoxyuridine phosphotriesters which incorporate enzyme mediated bioreversible protection such as S-acetylthioethanol (SATE) or dithiodiethanol (DTE) resulted in intracellular delivery of the parent mononucleotide. This point was corroborated by observation of an anti-HIV effect in various cell lines and decomposition data in cell extracts.
引用
收藏
页码:2521 / 2526
页数:6
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