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Mechanistic Insight into Antiretroviral Potency of 2'-Deoxy-2'-β-fluoro-4'-azidocytidine (FNC) with a Long-Lasting Effect on HIV-1 Prevention. 2020
Li Sun, and
Youmei Peng, and
Wenquan Yu, and
Yan Zhang, and
Lan Liang, and
Chuanjun Song, and
Jiao Hou, and
Yan Qiao, and
Qingduan Wang, and
Jingyu Chen, and
Mengli Wu, and
Dongwei Zhang, and
Ertong Li, and
Zhifu Han, and
Qingxia Zhao, and
Xia Jin, and
Bailing Zhang, and
Zhiwei Huang, and
Jijie Chai, and
Jian-Hua Wang, and
Junbiao Chang
Henan Key Laboratory of Organic Functional Molecule and Drug Innovation, College of Life Science, Henan Normal University, Xinxiang 453007, China.
In preclinical and phase I and II clinical studies, 2'-deoxy-2'-β-fluoro-4'-azidocytidine (FNC) displays a potent and long-lasting inhibition of HIV-1 infection. To investigate its mechanism of action, we compared it with the well-documented lamivudine (3TC). Pharmacokinetic studies revealed that the intracellular retention of FNC triphosphate in peripheral blood mononuclear cells was markedly longer than that of the 3TC triphosphate. FNC selectively enters and is retained in HIV target cells, where it exerts long-lasting prevention of HIV-1 infection. In addition to inhibition of HIV-1 reverse transcription, FNC also restores A3G expression in CD4+ T cells in FNC-treated HIV-1 patients. FNC binds to the Vif-E3 ubiquitin ligase complex, enabling A3G to avoid Vif-induced ubiquitination and degradation. These data reveal the mechanisms underlying the superior anti-HIV potency and long-lasting action of FNC. Our results also suggest a potential clinical application of FNC as a long-lasting pre-exposure prophylactic agent capable of preventing HIV infection.
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