【摘要】 艾滋病已在世界范围内给人类健康和社会发展带来了严重影响。抑制HIV-1与细胞膜融合的多肽抑制剂由于其分子量小、结构简单、生物毒性低和作用效果明显等优点而受到研究者的重视。针对HIV-1与细胞的融合过程中涉及gp160的分裂、gp120与CD4受体及辅助受体的结合、gp41自身的折叠及与细胞膜的并列与融合等步骤,可以设计一些新的多肽药物靶点,以达到阻止HIV-1侵入的目的。目前针对上述三步骤已分别设计出了相应的多肽抑制剂,如M3、HRPs、CD4M、S肽、DAPTA及C22等,这些多肽抑制剂在体外实验、动物实验或临床实验中均表现出较好的抑制HIV-1与细胞融合的能力,具有十分巨大的潜在应用前景。更多还原

【Abstract】 The quick spread of AIDS damages human health and social economy seriously.Now the anti-HIV drug researches focus on the inhibition of HIV-1 cell entry.Peptide inhibitors of HIV-1 cell fusion are a group of molecules with low molecular weight,simple structure,and low toxicity to human.HIV-1 cell fusion is the result of the process of split of gp160,the binding of gp120 with CD4 receptor and its coreceptor,the conformation change of gp41 and the membrane fusion with cell.The peptide inhibitors are designed in each step.A number of promising peptide inhibitors has been commenced clinical trials,including M3,HRPs,CD4M,S-peptide,DAPTA and C22.The activity of these peptides was studied by in vivo and in vitro tests.The reaction mechanisms and the potent future application were introduced.更多还原