Erastin

Erastin

Erastin is a small molecule that induces a form of non-apoptotic cell death known as ferroptosis. It was first identified in a high-throughput chemical screen for compounds that have selective lethality for oncogenic RAS-mutant cells.

Mechanism of Action

Erastin's mechanism of action is unique and complex. It functions by inhibiting the cystine/glutamate antiporter system Xc-, which is responsible for the import of cystine into the cell. Cystine is a crucial component of glutathione, an antioxidant that protects cells from oxidative stress. By inhibiting system Xc-, erastin depletes the cell of glutathione, leading to an accumulation of reactive oxygen species (ROS) and ultimately, ferroptosis.

Therapeutic Potential

Due to its ability to selectively kill RAS-mutant cells, erastin has potential therapeutic applications in the treatment of cancer. RAS mutations are common in many types of cancer, including pancreatic, lung, and colorectal cancers. However, the therapeutic potential of erastin is currently limited by its poor solubility and bioavailability.

Research

Research into erastin and ferroptosis is ongoing, with studies investigating the role of ferroptosis in various diseases, the development of erastin analogs with improved solubility and bioavailability, and the potential for combination therapies involving erastin and other anticancer agents.

See Also

• Ferroptosis
• RAS (gene)
• Glutathione
• Reactive oxygen species