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The development of anti-HIV agents targeting APOBEC3G/Vif axis
Qiqi Bao1, Jiajia Wen2, Fengjiao Xiang1
1Key Laboratory of the Ministry of Education for Advanced Catalysis Materials, Department of Chemistry, Zhejiang Normal University, 688 Yingbin Road, Jinhua 321004, China.
Bioorganic & Medicinal Chemistry
|December 19, 2025
Summary
Researchers developed new compounds that protect APOBEC3G (A3G), a protein that fights HIV-1 replication, from viral degradation. These compounds enhance A3G
Area of Science:
- Virology
- Molecular Biology
- Drug Discovery
Background:
- APOBEC3G (Apolipoprotein B mRNA editing enzyme-catalytic polypeptide-like 3G, A3G) is a human host restriction factor that inhibits human immunodeficiency virus type 1 (HIV-1) replication.
- HIV-1 viral infectivity factor (Vif) counteracts A3G by mediating its degradation, thereby abrogating its antiviral activity.
Purpose of the Study:
- To structurally optimize IMB-301, a previously identified compound that protects A3G from Vif-induced degradation.
- To develop novel anti-HIV-1 therapeutic strategies and candidate molecules.
Main Methods:
- Virtual screening and biological validation to identify IMB-301.
- Structural optimization of IMB-301, generating 64 analogs.
- Assessment of A3G protection, Vif-A3G interaction blocking, intracellular A3G levels, and HIV-1 proliferation inhibition.
Main Results:
- Most IMB-301 analogs retained HIV-1 inhibitory activity, with several showing enhanced potency.
- Active analogs effectively blocked the Vif-A3G interaction and restored intracellular A3G levels.
- These compounds inhibited HIV-1 proliferation in an A3G-dependent manner.
Conclusions:
- Structurally optimized analogs of IMB-301 demonstrate potent anti-HIV-1 activity by preserving A3G's antiviral function.
- This study highlights a promising therapeutic strategy for developing novel anti-HIV-1 agents.
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