Department of Cancer Immunology and Virology, Dana-Farber Cancer Institute, Boston, Massachusetts.
Center for Immunology and Inflammatory Diseases, Division of Rheumatology, Allergy and Immunology, Massachusetts General Hospital, Boston, Massachusetts.
J Infect Dis. 2018 Jul 2;218(3):471-475. doi: 10.1093/infdis/jiy174.
Small-molecule CD4-mimetic compounds (CD4mc) inhibit human immunodeficiency virus (HIV-1) entry by blocking binding to the CD4 receptor and by premature triggering of the viral envelope glycoprotein (Env) spike.
The efficacy of a CD4mc in protecting bone marrow-liver-thymus (BLT) humanized mice from vaginal HIV-1 challenge was evaluated.
Intravaginal application of the CD4mc JP-III-48, either before or simultaneously with virus challenge, protected BLT humanized mice from HIV-1JR-CSF infection in a dose- dependent manner.
The direct antiviral effects of a CD4mc prevent HIV-1 infection in a murine model of sexual transmission.
小分子 CD4 模拟化合物(CD4mc)通过阻断与 CD4 受体的结合以及过早触发病毒包膜糖蛋白(Env)刺突来抑制人类免疫缺陷病毒(HIV-1)的进入。
评估了一种 CD4mc 在保护骨髓-肝-胸腺(BLT)人源化小鼠免受阴道 HIV-1 攻击中的功效。
阴道内应用 CD4mc JP-III-48,无论是在病毒攻击之前还是同时应用,均能以剂量依赖的方式保护 BLT 人源化小鼠免受 HIV-1JR-CSF 感染。
CD4mc 的直接抗病毒作用可防止性传播小鼠模型中的 HIV-1 感染。