Chemistry:Erastin
From HandWiki
Erastin is a small molecule capable of initiating ferroptotic cell death.[1] Erastin binds and activates voltage-dependent anion channels (VDAC) by reversing tubulin's inhibition on VDAC2 and VDAC3,[2] and functionally inhibits the cystine-glutamate antiporter enzyme SLC7A11[3] Cells treated with erastin are deprived of cysteine and are unable to synthesize the antioxidant glutathione. Depletion of glutathione eventually leads to excessive lipid peroxidation and cell death.
Erastin was first described in 2003. Its name is short for "eradicator of RAS and ST-expressing cells".[4]
References
- ↑ "Ferroptosis: an iron-dependent form of nonapoptotic cell death". Cell 149 (5): 1060–1072. May 2012. doi:10.1016/j.cell.2012.03.042. PMID 22632970.
- ↑ "RAS-RAF-MEK-dependent oxidative cell death involving voltage-dependent anion channels". Nature 447 (7146): 864–868. June 2007. doi:10.1038/nature05859. PMID 17568748. Bibcode: 2007Natur.447..865Y.
- ↑ "Pharmacological inhibition of cystine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis". eLife 3. May 2014. doi:10.7554/elife.02523. PMID 24844246.
- ↑ "Identification of genotype-selective antitumor agents using synthetic lethal chemical screening in engineered human tumor cells". Cancer Cell 3 (3): 285–296. March 2003. doi:10.1016/S1535-6108(03)00050-3. PMID 12676586.
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