De Clercq E
Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium.
Chemioterapia. 1988 Dec;7(6):357-64.
Several steps in the replicative cycle of human immunodeficiency virus (HIV) could be envisaged as targets for anti-AIDS drugs. The anionic compound PMEA [9-(2-phosphonyl-methoxyethyl)adenine], the 2'3'-dideoxynucleoside analogues D4T (2',3-deidehydro-2',3'-dideoxythymidine), AzddUrd 3'-azido-2',3'-dideoxyuridine), FddUrd (3'-fluoro-2',3-dideoxyuridine), AzddDAPR (3'-azido-2',3'-dideoxy-2,6' diaminopurine riboside) and the sulfated polysaccharides dextran sulfate and pentosan polysulfate are among the most promising candidate anit-AIDS drugs which have been recently described. They are targeted at either virus-cell binding (dextran sulfate, pentosan polysulfate) or virus-associated reverse transcriptase (PMEA, D4T, AzddUrd, FddUrd, AzddDAPR).
人类免疫缺陷病毒(HIV)复制周期中的几个步骤可以被设想为抗艾滋病药物的作用靶点。阴离子化合物PMEA [9-(2-膦酰甲氧基乙基)腺嘌呤]、2'3'-双脱氧核苷类似物D4T(2',3-双脱氢-2',3'-双脱氧胸苷)、叠氮脱氧胸苷(3'-叠氮-2',3'-双脱氧尿苷)、氟脱氧尿苷(3'-氟-2',3-双脱氧尿苷)、叠氮双脱氧二氨基嘌呤核苷(3'-叠氮-2',3'-双脱氧-2,6'-二氨基嘌呤核糖苷)以及硫酸化多糖硫酸葡聚糖和硫酸戊聚糖是最近描述的最有前景的候选抗艾滋病药物。它们的作用靶点要么是病毒与细胞的结合(硫酸葡聚糖、硫酸戊聚糖),要么是病毒相关的逆转录酶(PMEA、D4T、叠氮脱氧胸苷、氟脱氧尿苷、叠氮双脱氧二氨基嘌呤核苷)。