中文摘要：

新讲道理地设计的 i，指向 HIV-1 汇编和入口的 i+7-hydrocarbon-stapled 肽被显示了对在欧洲和北美洲传播的 HIV-1 子类型举办抗病毒的活动。这里，我们试图把这些肽的抗病毒的活动与主要在三 i， i+7-hydrocarbon-stapled 肽， NYAD-36， NYAD-67，和 NYAD-66 的 China.MethodsThe 抗病毒的活动传播的 HIV-1 子类型作比较，对主要 HIV-1 CRF07_BC 和 CRF01_AE 孤立在外部血 mononuclear 房间(PBMC ) 被评估。对 CRF07_BC 和 CRF01_AE Env-pseudotyped 病毒的活动在发现的 TZM-bl cells.ResultsWe 被分析所有 stapled 肽在由主要 HIV-1 孤立的所有禁止感染是有效的，这测试了，与向病毒的复制的 50% 禁止的集中(在低 micromolar 范围的 IC ₅₀) 。NYAD-36 和 NYAD-67 比 NYAD-66 显示出更好抗病毒的活动。我们进一步在单个周期的病毒传染性试金评估了 CRF01_AE 和 CRF07_BC Env-pseudotyped 病毒的敏感到这些 stapled 肽。是观察了与主要孤立， IC ₅₀ s 在低 micromolar 范围，并且 NYAD-66 比 NYAD-36 和 NYAD-67.ConclusionHydrocarbon-stapled 肽看起来在中国对占优势的 HIV-1 病毒举办宽广抗病毒的活动的是不太有效的。这发现可以为未来提供动力给肽的合理设计抗病毒的治疗。

英文摘要：

Objective New rationally designed i,i＋7-hydrocarbon-stapled peptides that target both HIV-1 assembly and entry have been shown to have antiviral activity against HIV-1 subtypes circulating in Europe and North America. Here, we aimed to evaluate the antiviral activity of these peptides against HIV-1 subtypes predominantly circulating in China. Methods The antiviral activity of three i,i＋7-hydrocarbon-stapled peptides, NYAD-36, NYAD-67, and NYAD-66, against primary HIV-1 CRF07_BC and CRFOI_AE isolates was evaluated in peripheral blood mononuclear cells （PI3MCs）. The activity against the CRF07_BC and CRF01_AE Env-pseudotyped viruses was analyzed in TZM-bl cells. Results We found that all the stapled peptides were effective in inhibiting infection by all the primary HIV-1 isolates tested, with 50% inhibitory concentration toward viral replication （ICso） in the low micromolar range. NYAD-36 and NYAD-67 showed better antiviral activity than NYAD-66 did. We further evaluated the sensitivity of CRF01_AE and CRF07_BC Env-pseudotyped viruses to these stapled peptides in a single-cycle virus infectivity assay. As observed with the primary isolates, the ICs0s were in the low micromolar range, and NYAD-66 was less effective than NYAD-36 and NYAD-67. Conclusion Hydrocarbon-stapled peptides appear to have broad antiviral activity against the predominant HIV-1 viruses in China. This finding may provide the impetus to the rational design of peptides for future antiviral therapy.