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Updated: May 31, 2026

High-throughput Antiviral Assays to Screen for Inhibitors of Zika Virus Replication
Published on: October 30, 2021
Computational Drug Repurposing Predicts FDA-Approved Drugs as Potential Inhibitors of Chikungunya Virus nsP2 Protease
Quynh Mai Thai1,2, Huong Thi Thu Phung3,4, Son Tung Ngo1,2
1Laboratory of Biophysics, Institute for Advanced Study in Technology, Ton Duc Thang University, Ho Chi Minh City 72915, Vietnam.
Abstract:
Chikungunya virus (CHIKV) infection remains a significant global health threat with no approved specific antiviral therapy. The nonstructural protein 2 protease (nsP2pro) is essential for viral replication and represents an attractive target for structure-based drug design. In this study, we employed a computational drug repurposing strategy to predict potential nsP2pro inhibitors from FDA-approved compound libraries. We performed molecular docking screens of 1820 unique compounds against the nsP2pro active site. The eight selected top-scoring compounds had docking scores better than that of the reference inhibitor pantinin-1. Subsequent molecular dynamics (MD) simulations revealed that, except for lomitapide, which dissociated from the pocket, the remaining leads formed dynamically stable complexes and modulated the catalytic environment in a chemotype-dependent manner. Small molecules expanded both the Cys478-His548 and Ser482-His548 distances, consistent with dyad perturbation, whereas GnRH-like peptides preserved a more compact geometry in the modeled noncovalent complexes, pointing to possible nonproductive occupation of the active-site region. Free energy perturbation calculations further provided a relative energetic ranking that supported the MD-derived mechanistic trends and placed six compounds ahead of pantinin-1 within the present data set. Among the small-molecule candidates, venetoclax and lapatinib emerge as computationally prioritized candidates for future biochemical and antiviral evaluation. Overall, this study provides mechanistic insight into noncovalent recognition of CHIKV nsP2pro and a framework for future experimental validation.

