Erastin is a small molecule capable of initiating ferroptotic cell death. Erastin binds and activates voltage-dependent anion channels (VDAC) by reversing tubulin's inhibition on VDAC2 and VDAC3, and functionally inhibits the cystine-glutamate

antiporter An antiporter (also called exchanger or counter-transporter) is an integral membrane protein that uses secondary active transport to move two or more molecules in opposite directions across a phospholipid membrane. It is a type of cotransporte ...

enzyme

SLC7A11 Cystine/glutamate transporter is an antiporter that in humans is encoded by the ''SLC7A11'' gene. The ''SLC7A11'' gene encodes a sodium-independent cystine-Glutamate (neurotransmitter), glutamate antiporter that is chloride dependent, also know ...

Cells treated with erastin are deprived of

cysteine Cysteine (; symbol Cys or C) is a semiessential proteinogenic amino acid with the chemical formula, formula . The thiol side chain in cysteine enables the formation of Disulfide, disulfide bonds, and often participates in enzymatic reactions as ...

and are unable to synthesize the antioxidant

glutathione Glutathione (GSH, ) is an organic compound with the chemical formula . It is an antioxidant in plants, animals, fungi, and some bacteria and archaea. Glutathione is capable of preventing damage to important cellular components caused by sources ...

. Depletion of glutathione eventually leads to excessive

lipid peroxidation Lipid peroxidation, or lipid oxidation, is a complex chemical process that leads to oxidative degradation of lipids, resulting in the formation of peroxide and hydroperoxide derivatives.{{Cite journal , last1=Ayala , first1=Antonio , last2=Muñoz ...

and

cell death Cell death is the event of a biological cell ceasing to carry out its functions. This may be the result of the natural process of old cells dying and being replaced by new ones, as in programmed cell death, or may result from factors such as di ...

. Erastin was first described in 2003. Its name is short for "eradicator of RAS and ST-expressing cells".

References

Experimental drugs 4-Chlorophenyl compounds Piperazines Phenol ethers {{pharma-stub