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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\u2014both inducers and inhibitors\u2014that target the mechanisms of ferroptosis, particularly in the field of anti\u2010tumor drug research. This review systematically elucidates the regulatory mechanisms underlying ferroptosis (e.g., iron metabolism, lipid peroxidation, system Xc\n                    <jats:sup>\u2212<\/jats:sup>\n                    \/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\u2010related diseases.\n                  <\/jats:p>","DOI":"10.1002\/med.70034","type":"journal-article","created":{"date-parts":[[2026,3,8]],"date-time":"2026-03-08T17:29:44Z","timestamp":1772990984000},"page":"853-895","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":1,"title":["Accelerating Small Molecule Ferroptosis Regulator Development With Advances in Biological Functions"],"prefix":"10.1002","volume":"46","author":[{"given":"Linyue","family":"Bai","sequence":"first","affiliation":[{"name":"State Key Laboratory of Metabolic Dysregulation &amp; prevention and Treatment of Esophageal Cancer, Key Laboratory of Advanced Drug preparation Technologies, Ministry of Education, Key Laboratory of Henan Province for Small Molecule Drug Discovery and Application, School of Pharmaceutical Sciences Zhengzhou University Zhengzhou China"},{"name":"Department of Pharmacy The First People's Hospital of Dali Dali China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Liang","family":"Shen","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Metabolic Dysregulation &amp; prevention and Treatment of Esophageal Cancer, Key Laboratory of Advanced Drug preparation Technologies, Ministry of Education, Key Laboratory of Henan Province for Small Molecule Drug Discovery and Application, School of Pharmaceutical Sciences Zhengzhou University Zhengzhou China"},{"name":"Jiang Su Key Laboratory of Drug Design and Optimization and state key Laboratory of Natural Medicines China pharmaceutical University Nanjing China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Qianqian","family":"Zhang","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Metabolic Dysregulation &amp; prevention and Treatment of Esophageal Cancer, Key Laboratory of Advanced Drug preparation Technologies, Ministry of Education, Key Laboratory of Henan Province for Small Molecule Drug Discovery and Application, School of Pharmaceutical Sciences Zhengzhou University Zhengzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Zhuang","family":"Hu","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Metabolic Dysregulation &amp; prevention and Treatment of Esophageal Cancer, Key Laboratory of Advanced Drug preparation Technologies, Ministry of Education, Key Laboratory of Henan Province for Small Molecule Drug Discovery and Application, School of Pharmaceutical Sciences Zhengzhou University Zhengzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yanjun","family":"Tang","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Metabolic Dysregulation &amp; prevention and Treatment of Esophageal Cancer, Key Laboratory of Advanced Drug preparation Technologies, Ministry of Education, Key Laboratory of Henan Province for Small Molecule Drug Discovery and Application, School of Pharmaceutical Sciences Zhengzhou University Zhengzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mengjie","family":"Fu","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Metabolic Dysregulation &amp; prevention and Treatment of Esophageal Cancer, Key Laboratory of Advanced Drug preparation Technologies, Ministry of Education, Key Laboratory of Henan Province for Small Molecule Drug Discovery and Application, School of Pharmaceutical Sciences Zhengzhou University Zhengzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yange","family":"Fan","sequence":"additional","affiliation":[{"name":"Institute of Chemistry Co. 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