HIV-associated morbidity and mortality have markedly declined because of combinational antiretroviral therapy, but HIV readily mutates to develop drug resistance. Developing antivirals against previously undefined targets is essential to treat existing drug-resistant HIV strains. Some peptides derived from HIV-1 envelope glycoprotein (Env, gp120-gp41) have been shown to be effective in inhibiting HIV-1 infection. Therefore, we screened a peptide library from HIV-1 Env and identified a peptide from the cytoplasmic region, designated F9170, able to effectively inactivate HIV-1 virions and induce necrosis of HIV-1–infected cells, and reactivated latently infected cells. F9170 specifically targeted the conserved cytoplasmic tail of HIV-1 Env and effectively disrupted the integrity of the viral membrane. Short-term monoadministration of F9170 controlled viral loads to below the limit of detection in chronically SHIV-infected macaques. F9170 can enter the brain and lymph nodes, anatomic reservoirs for HIV latency. Therefore, F9170 shows promise as a drug candidate for HIV treatment.

由于联合使用抗逆转录病毒疗法，与HIV相关的发病率和死亡率显着下降，但HIV容易发生突变以产生耐药性。针对先前不确定的目标开发抗病毒药物对于治疗现有的耐药HIV菌株至关重要。某些源自HIV-1包膜糖蛋白（Env，gp120-gp41）的肽已被证明可有效抑制HIV-1感染。因此，我们从HIV-1 Env中筛选了一个肽库，并从细胞质区域鉴定了一种肽，命名为F9170，该肽能够有效地灭活HIV-1病毒体并诱导被HIV-1感染的细胞坏死，并重新激活潜伏感染的细胞。F9170特别针对HIV-1 Env保守的细胞质尾巴，并有效破坏了病毒膜的完整性。在慢性SHIV感染的猕猴中，短期单次施用F9170可将病毒载量控制在检测限以下。F9170可以进入大脑和淋巴结，成为HIV潜伏期的解剖库。因此，F9170有望成为HIV治疗的候选药物。