Tuncal A, et al. Clinica Chimica Acta, 2024, 558, 118992.
This study evaluates bisacodyl as a candidate therapeutic compound targeting CHEK2-associated pathways in chondrosarcoma (CS). Using an in silico Drug Set Enrichment Analysis (DSEA) approach through the Gene2Drug platform, compounds were screened for gene-specific modulation. CHEK2, implicated in cell cycle regulation and cancer susceptibility, was selected as a potential therapeutic target based on genomic analyses of dedifferentiated CS.
Drug sensitivity profiling was conducted using PRISM Repurposing Primary data across eight CS cell lines. Among 593 screened agents, eight compounds demonstrated significant sensitivity (P < 1×10⁻³), with bisacodyl identified as a promising candidate. Mechanistically, bisacodyl is associated with G protein-coupled receptor 35 modulation, a class widely investigated in oncology. This study highlights bisacodyl's experimental application in computational drug repurposing pipelines combined with large-scale viability assays, supporting its potential utility in precision-targeted therapy for chondrosarcoma.