2019
DOI: 10.1016/j.chembiol.2019.01.008
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Abstract: Ferroptosis is a form of regulated cell death that can be induced by inhibition of the cystine-glutamate antiporter, system x c -. Among the existing system x c inhibitors, imidazole ketone erastin (IKE) is a potent, metabolically stable inhibitor of system x c and inducer of ferroptosis potentially suitable for in vivo applications. We investigated the pharmacokinetic and pharmacodynamic features of IKE in a diffuse large B cell lymphoma (DLBCL) xenograft model and demonstrated that IKE exerted an antitumor e… Show more

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Cited by 405 publications
(278 citation statements)
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“…Most recently, the water solubility and anticancer performance of erastins have been further improved by another metabolically stable erastin derivative, imidazole ketone erastin (IKE), with the solubility three times of erastin (0.25 × 10 −3 m ) and half‐maximal inhibitory concentration (IC 50 ) for BJeLR cells only 3 × 10 −9 m (Erastin BJeLR IC 50 is 625 × 10 −9 m ). IKE has been successfully applied for treating diffuse large B cell lymphoma (DLBCL) in SUDHL6 xenograft animal model (Figure C) …”
Section: Ferroptosis Inducers For Cancer Therapymentioning
confidence: 99%
See 1 more Smart Citation
“…Most recently, the water solubility and anticancer performance of erastins have been further improved by another metabolically stable erastin derivative, imidazole ketone erastin (IKE), with the solubility three times of erastin (0.25 × 10 −3 m ) and half‐maximal inhibitory concentration (IC 50 ) for BJeLR cells only 3 × 10 −9 m (Erastin BJeLR IC 50 is 625 × 10 −9 m ). IKE has been successfully applied for treating diffuse large B cell lymphoma (DLBCL) in SUDHL6 xenograft animal model (Figure C) …”
Section: Ferroptosis Inducers For Cancer Therapymentioning
confidence: 99%
“…For designing of nano ferroptosis inducers, an intuitional method is to incorporate small molecule ferroptosis inducers into nano delivery vehicles. Compared with free drugs, nanoplatforms enable improved solubility and biocompatibility, as well as increased tumor accumulation by either active or passive targeting . More appealingly, the mainstream research focuses on nanomaterials themselves which can induce ferroptosis by participating in biochemical reactions and interfering the metabolic balance.…”
Section: Ferroptosis Inducers For Cancer Therapymentioning
confidence: 99%
“…Whether these two agents cause GPX4 inactivation and how lipid peroxidation is affected at the molecular level are not clear. Most recently, treatment with the bioavailable erastin analogue imidazole ketone erastin (IKE) embedded within a biodegradable polyethylene glycol‐poly(lactic‐ co ‐glycolic acid) carrier reduced tumor burden in a xenograft model of diffuse large B cell lymphoma (DLBCL) . Protein adducts characteristic of enhanced lipid peroxidation were detected in tumors treated with this agent, consistent with increased lipid peroxidation.…”
Section: Gpx4 Lipid Peroxidation and Ferroptosis In Development Andmentioning
confidence: 99%
“…Many DLBCL cell lines are sensitive to ferroptosis because they lack the machinery to synthesize cysteine, a precursor for glutathione. In a mouse xenograft model of DLBCL, IKE slowed tumor growth and induced pharmacodynamic markers of ferroptosis: reduced levels of glutathione, increases in lipid peroxidation, and a genetic profile consistent with ferroptosis …”
Section: Inducing Cancer Cell Death Via Ferroptosismentioning
confidence: 99%
“…In a mouse xenograft model of DLBCL, IKE slowed tumor growth and induced pharmacodynamic markers of ferroptosis: reduced levels of glutathione, increases in lipid peroxidation, and a genetic profile consistent with ferroptosis. 27 Stockwell proposed that ferroptosis inducers can synergize with some other standard therapeutic regimens; work in this area is ongoing in the Stockwell Laboratory and may be published by the year's end. In addition, the laboratory is identifying biomarkers to predict which tumors will respond most sensitively to ferroptosis inducers.…”
Section: Inducing Cancer Cell Death Via Ferroptosismentioning
confidence: 99%