This article may be too technical for most readers to understand. (April 2017) |
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 system Xc−.[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.
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| Formula | C30H31ClN4O4 |
| Molar mass | 547.05 g·mol−1 |
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Erastin was first described in 2003. Its name is short for "eradicator of RAS and ST-expressing cells".[4]
References
edit- ^ Dixon SJ, Lemberg KM, Lamprecht MR, Skouta R, Zaitsev EM, Gleason CE, et al. (May 2012). "Ferroptosis: an iron-dependent form of nonapoptotic cell death". Cell. 149 (5): 1060–1072. doi:10.1016/j.cell.2012.03.042. PMC 3367386. PMID 22632970.
- ^ Yagoda N, von Rechenberg M, Zaganjor E, Bauer AJ, Yang WS, Fridman DJ, et al. (June 2007). "RAS-RAF-MEK-dependent oxidative cell death involving voltage-dependent anion channels". Nature. 447 (7146): 864–868. Bibcode:2007Natur.447..865Y. doi:10.1038/nature05859. PMC 3047570. PMID 17568748.
- ^ Dixon SJ, Patel DN, Welsch M, Skouta R, Lee ED, Hayano M, et al. (May 2014). "Pharmacological inhibition of cystine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis". eLife. 3: e02523. doi:10.7554/elife.02523. PMC 4054777. PMID 24844246.
- ^ Dolma S, Lessnick SL, Hahn WC, Stockwell BR (March 2003). "Identification of genotype-selective antitumor agents using synthetic lethal chemical screening in engineered human tumor cells". Cancer Cell. 3 (3): 285–296. doi:10.1016/S1535-6108(03)00050-3. PMID 12676586.
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