Figure 2.
Synergistic mechanisms of PD-1/PD-L1 inhibitors combined with ferroptosis inducers (and chemotherapy) against drug-resistant cancer. Left: PD-L1 overexpression on drug-resistant cancer cells binds to PD-1 on CD8+ T effector cells, transmitting inhibitory signals to suppress T cell activity. PD-1/PD-L1 inhibitors block this interaction, restoring CD8+ T cell function—activated CD8+ T cells secrete IFNγ, which upregulates ACSL4 (by 2.8-fold) to promote PUFA-CoA synthesis. LPCAT3 esterifies PUFA-CoA into PUFA-PLs (lipid peroxidation substrates), enhancing ferroptosis sensitivity. Middle: Ferroptosis inducers target key antioxidant pathways—Erastin inhibits System Xc- (blocking cystine uptake, reducing GSH synthesis), while RSL3 directly inhibits GPX4 (impairing PLOOH clearance). Drug-resistant cancer cells with high SLC7A11 expression exhibit ferroptosis resistance, which is reversed by the combined action of immunotherapy and ferroptosis inducers. Right: Immunosuppressive factors in the tumor microenvironment—M2-type tumor-associated macrophages (TAMs) secrete IL-10 to upregulate GSTP1 (enhancing antioxidant defense, suppressing ferroptosis). Bottom: Joint chemotherapy strategy (DAT + Cisplatin): DAT expands the labile iron pool (LIP) via TfR1 to promote Fenton reaction-mediated •OH generation; Cisplatin induces DNA damage and ROS accumulation, synergizing with ferroptosis to kill drug-resistant cancer cells.
