From Bitter Taste Perception to Anti-Cancer Weapons: New Directions for Bitter Taste Receptors in Malignant Tumor Treatment.

Cancer heterogeneity and drug resistance remain major challenges in current treatments. Bitter taste receptors (TAS2Rs), as members of the G protein-coupled receptor family, have demonstrated significant roles in tumor research in recent years. TAS2Rs are differentially expressed in various cancer cells and influence processes such as cell cycle progression, apoptosis, migration, and invasion by regulating intracellular Ca²⁺ concentrations. Their activation inhibits tumor proliferation, promotes apoptosis, and regulates angiogenesis, immune inflammation, and gut microbiota balance within the tumor microenvironment. Emerging evidence suggests that TAS2R expression is tightly regulated by epigenetic mechanisms, transcription factors, and microRNAs, and that genetic polymorphisms in TAS2Rs may influence cancer susceptibility and therapeutic outcomes. Several natural products (such as saikosaponins, scutellarin, etc.) can specifically activate TAS2Rs, demonstrating antitumor potential. However, the mechanisms regulating TAS2R expression remain unclear, and the complex composition of natural products limits their clinical application. Future research should focus on elucidating the mechanisms of action of TAS2Rs, determining their ligand structures, and advancing high-quality clinical trials to facilitate the translational application of TAS2R-targeted therapies in oncology.