Tsibinogin V V, Kraevskiĭ A A, Bibilashvili R Sh, Gren E Ia, Kiselev L L
Mol Biol (Mosk). 1989 Jul-Aug;23(4):983-7.
Several nucleoside 5'-triphosphate analogs were investigated as inhibitors of human hepatitis B virus replication. Different analogs inhibited DNA synthesis differently, 3'-azido-2',3'-dideoxythymidine 5'triphosphate being the most active compound. This inhibitor blocked DNA synthesis by 50% at inhibitor: substrate molar ratio 1:8, and by 80% - at 1:1. The hypothesis is formulated that 3'-azido-2',3'-dideoxythymidine 5'-triphosphate inhibits RNA directed viral DNA replication due to incorporation of this compound into 3'-termini of newly synthesized DNA chains. The phenomenon observed opens new possibilities for chemotherapy of acute and chronic human hepatitis B.
研究了几种核苷5'-三磷酸类似物作为人乙型肝炎病毒复制抑制剂的作用。不同的类似物对DNA合成的抑制作用不同,3'-叠氮-2',3'-双脱氧胸苷5'-三磷酸是最具活性的化合物。该抑制剂在抑制剂与底物摩尔比为1:8时可使DNA合成受阻50%,在1:1时可使DNA合成受阻80%。提出的假设是,3'-叠氮-2',3'-双脱氧胸苷5'-三磷酸通过将该化合物掺入新合成的DNA链的3'-末端来抑制RNA指导的病毒DNA复制。观察到的这一现象为急性和慢性人类乙型肝炎的化疗开辟了新的可能性。