Transcriptomic profiling of colorectal cancer cells treated with the dual-targeting TOP1/G4 inhibitor ZBH-01

This study employs RNA sequencing to investigate the transcriptomic changes induced by ZBH-01, a camptothecin derivative that dual inhibits topoisomerase I (TOP1) and stabilizes DNA G-quadruplexes (G4s), in colorectal cancer (CRC) cells. The dataset includes profiles from the human colorectal adenocarcinoma cell line LS174T, treated with ZBH-01, its parent compound irinotecan (CPT-11), and its active metabolite SN-38. Analyses reveal that ZBH-01 triggers broad transcriptional alterations, significantly downregulating genes involved in cell cycle progression, DNA replication, and telomere maintenance (e.g., hTERT, MYC), while upregulating pathways associated with cellular senescence and DNA damage response. These findings provide genome-wide insights into how concurrent targeting of TOP1 and oncogenic G4 structures synergistically disrupts survival mechanisms and overcomes chemoresistance in CRC. The data support the manuscript titled 'Dual Targeting of Topoisomerase I and DNA G-Quadruplexes Enhances Senescence and Chemosensitivity in Colorectal Cancer.'