Acta Pharmaceutica Sinica B
|
2026, 16(6): 3784-3801
• Original articles •
VPS34 inhibition as a host-targeting anti-coronaviral strategy: Rational design of YBM with optimized pharmacokinetic parameters
Full
Chenchen Ge1, Zihao Wang2, Zhiwei Zhao3, Xiaoyu Zhang1, Xiaoyang Yu1, Minghua Chen1, Kai Liu1, Lisen Lin1, Dapeng Li1, Ningyi Jin1, Peifu Jiao2, Shiyong Fan2, Chao Shang1, Xiao Li1
Affiliations
1 Changchun Veterinary Research Institute, Chinese Academy of Agricultural Sciences, Changchun 130122, China;
2 National Engineering Research Center for the Emergency Drug, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China;
3 College of Life Sciences, Shandong Normal University, Jinan 250014, China
doi: 10.1016/j.apsb.2025.12.020
Outline
Targeting host factors critical to the viral life cycle instead of direct viral enzyme inhibition represents a promising alternative strategy for developing broad-spectrum antivirals. Here, we identified VPS34, a key regulator of autophagosome-lysosome fusion and membrane trafficking, as a conserved host-dependency factor across coronaviruses. VPS34 gene knockdown significantly attenuates viral replication both in vitro and in vivo. Crucially, this antiviral effect remained potent against emerging severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) variants, demonstrating that VPS34 is a drug target resilient to viral evolution. Based on the scaffold structure of the VPS34 inhibitor SAR405, we developed YBM, a novel small-molecule inhibitor, via critical group substitutions and aliphatic chain introduction. YBM exhibited superior pharmacokinetic properties than SAR405, including enhanced bioavailability and prolonged plasma half-life. YBM shows significant in vivo efficacy against SARS-CoV-2 and HCoV-OC43. Crucially, its broad-spectrum potential is underscored by potent in vitro activity against multiple coronavirus genera (α and γ). This study established YBM as a host-targeting antiviral (HTA) that targets VPS34, offering protection against both extant and evolving coronaviruses. The evolutionarily conserved role of VPS34 in mediating coronavirus replication suggests that this host factor may become a priority therapeutic target for coronaviruses during future pandemics.
Host-targeting antivirals
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Broad-spectrum anti-coronavirus
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SARS-CoV-2
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HCoV-OC43
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VPS34
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In vivo
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Pharmacokinetics
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Inhibitors
Chenchen Ge, Zihao Wang, Zhiwei Zhao, Xiaoyu Zhang, Xiaoyang Yu, Minghua Chen, Kai Liu, Lisen Lin, Dapeng Li, Ningyi Jin, Peifu Jiao, Shiyong Fan, Chao Shang, Xiao Li.
VPS34 inhibition as a host-targeting anti-coronaviral strategy: Rational design of YBM with optimized pharmacokinetic parameters[J].
Acta Pharmaceutica Sinica B,
2026
, 16
(6)
: 3784
-3801
.
DOI: 10.1016/j.apsb.2025.12.020
Year 2026 volume 16 Issue 6
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Article Info
doi: 10.1016/j.apsb.2025.12.020
- Receive Date:2025-07-25
- Online Date:2026-09-17