Accelerating Small Molecule Ferroptosis Regulator Development With Advances in Biological Functions

ABSTRACT Ferroptosis is an iron‐dependent cell death characterized by the disorder of iron homeostasis and the accumulation of lipid peroxidation, which trigger a cascade of events resulting in cell death. This process has a dual regulatory effect in the evolution of diseases, which can not only attenuate the progress of diseases, but also become a promoting force to accelerate pathological alterations, and widely participate in the occurrence and development of multiple diseases. In recent years, there has been a growing body of research identifying regulators—both inducers and inhibitors—that target the mechanisms of ferroptosis, particularly in the field of anti‐tumor drug research. This review systematically elucidates the regulatory mechanisms underlying ferroptosis (e.g., iron metabolism, lipid peroxidation, system Xc − /GSH/GPX4 axis) and examines the role of ferroptosis in the pathogenesis of various diseases, such as cancer, neurodegenerative diseases, liver and kidney diseases, and cardiovascular diseases. Additionally, we discussed the therapeutic applications of novel inducers and inhibitors of ferroptosis in recent years, offering critical insights and directions for further researching on the mechanism of ferroptosis and targeted drugs for ferroptosis‐related diseases.