International Journal of Molecular Sciences
Reporter Virus-Based High-Throughput Screening Identifies LM-10 as a Novel Inhibitor Targeting KRM1 for Coxsackievirus A10 Blockade
By Haimeng Li, Wenrui Gai, Hailan Yao and 9 others.
Abstract
Enteroviruses causing hand, foot, and mouth disease, including currently circulating Coxsackievirus A10 (CVA10) and Coxsackievirus A6 (CVA6), rely on KREMEN1 (KRM1) for cell entry, making the virus–KRM1 interface a potential target for antiviral intervention. We screened GLMarNP, an in-house library of about 3000 natural products and derivatives. Candidates targeting the KRM1 ectodomain were selected by blind docking, drug-likeness assessment, and scaffold diversity analysis. To enable high-throughput antiviral screening, we inserted eGFP into a full-length infectious CVA10 cDNA clone to generate a reporter virus designated eGFP-A10. The virus was rescued in HEK293T cells and produced robust fluorescence in RD cells over serial passages. Among 29 candidate compounds, LM-10 showed the strongest antiviral activity and exhibited low cytotoxicity. Mechanistically, LM-10 bound KRM1 and acted early in the viral life cycle. Molecular docking suggested that LM-10 binds the KR domain at a site overlapping the VP2 EF-loop contact region. KRM1 also acts as a DKK1 receptor to regulate Wnt/β-catenin signaling. LM-10 did not significantly affect this pathway in the TOP-GFP reporter assay or in transgenic zebrafish embryos. These findings establish a practical CVA10 reporter-virus platform and support steric blockade of the receptor interface as a potential antiviral strategy.



