Ferroptosis inducers – erastin and analogues (review)

• Published in: Razrabotka i registraciâ lekarstvennyh sredstv (Online) Vol. 13; no. 2; pp. 77 - 83
• Main Authors: Sanarova, E. V., Lantsova, A. V., Nikolaeva, L. L., Oborotova, N. A., Borisova, L. M.
• Format: Journal Article
• Language: English; Russian
• Published: LLC Center of Pharmaceutical Analytics (LLC «CPHA») 01.06.2024
• Subjects: antitumour effect; erastin; erastin analogues; ferroptosis; reactive oxygen species
• ISSN: 2305-2066; 2658-5049
• DOI: 10.33380/2305-2066-2024-13-2-1786

Introduction. Improving the efficacy of chemotherapy is a non-trivial task of modern oncology. Its successful solution requires knowledge in many fields, including physiology, pathology, clinical oncology, pharmacology and others. The search for small molecules that selectively kill tumor cells led to the accidental discovery of erastin. Text. Erastin is a unique molecule that has a quinazoline fragment in its structure. Not so long ago it became known that the antitumour effect of this compound is due to the induction of ferroptosis – an iron-dependent form of cell death caused by lipid peroxidation. Erastin is able to induce ferroptosis through various biochemical pathways, including blocking of cystine-glutamate transport channel of cell membrane and potential-dependent anion channel of mitochondria, as well as activation of p53 protein. Conclusion. Pharmacological induction of ferroptosis by erastin and its analogues represents a promising direction in cancer chemotherapy. In addition, erastin and its analogues are able to increase sensitivity to chemotherapy and radiation therapy, which allows us to talk about the possibility of their use in the combined treatment of malignant neoplasms.