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Imidazole ketone erastin induces ferroptosis and slows tumor growth in a mouse lymphoma model - PMC

pmc.ncbi.nlm.nih.gov · 8,948 words · saved by 1 readers

Ferroptosis is a form of regulated cell death that can be induced by inhibition of the cystine-glutamate antiporter, system xc−. Among the existing system xc− inhibitors, imidazole-ketone-erastin (IKE) is a potent, metabolically stable inhibitor of ...

. Author manuscript; available in PMC: 2020 May 16. SUMMARY Ferroptosis is a form of regulated cell death that can be induced by inhibition of the cystine-glutamate antiporter, system xc−. Among the existing system xc− inhibitors, imidazole-ketone-erastin (IKE) is a potent, metabolically stable inhibitor of system xc− and inducer of ferroptosis potentially suitable for in vivo applications. We investigated the pharmacokinetics and pharmacodynamics for IKE in a diffuse large B cell lymphoma (DLBCL) xenograft model and demonstrated that IKE exerted an antitumor effect by inhibiting system…

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