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Structure–activity relationships of GPX4 inhibitor warheads

Direct inhibition of GPX4 requires covalent modification of the active-site selenocysteine. While phenotypic screening has revealed that activated alkyl chlorides and masked nitrile oxides can inhibit GPX4 covalently, a systematic assessment of potential electrophilic warheads with the capacity to i...

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Bibliographic Details
Published in:Bioorg Med Chem Lett
Main Authors: Eaton, John K., Furst, Laura, Cai, Luke L., Viswanathan, Vasanthi S., Schreiber, Stuart L.
Format: Artigo
Language:Inglês
Published: 2020
Subjects:
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC8006158/
https://ncbi.nlm.nih.gov/pubmed/32920142
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2020.127538
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