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VPS34 inhibition as a host-targeting anti-coronaviral strategy: Rational design of YBM with optimized pharmacokinetic parameters
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Acta Pharmaceutica Sinica B | 2026, 16(6) : 3784 - 3801
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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
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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
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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  /  Broad-spectrum anti-coronavirus  /  SARS-CoV-2  /  HCoV-OC43  /  VPS34  /  In vivo  /  Pharmacokinetics  /  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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doi: 10.1016/j.apsb.2025.12.020
  • Receive Date:2025-07-25
  • Online Date:2026-09-17
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  • Received:2025-07-25
  • Revised:2025-10-16
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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