
NCBI . NLM . NIH . GOV {
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Title[redir]:
Selective covalent targeting of GPX4 using masked nitrile-oxide electrophiles - PMC
Description:
We recently described GPX4 as a promising target for killing therapy-resistant cancer cells via ferroptosis. Remarkably, the induction of therapy resistance by multiple types of treatments results in a stable cell state marked by high levels of ...
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Keywords {🔍}
gpx, fig, cells, jke, supplementary, inhibitors, google, scholar, cell, doi, pubmed, cellular, pmc, compounds, covalent, article, nitrileoxide, free, ferroptosis, chloroacetamide, chem, nitrile, cancer, protein, masked, data, experiments, group, selectivity, loximvi, mass, rsl, adduct, final, chemical, activity, treated, dmso, oxides, reactivity, assay, lipid, samples, performed, nitrolic, biol, cetsa, reaction, concentration, shown,
Topics {✒️}
decaprenylphosphoryl-beta-d-ribose 2’-epimerase dpre1 copper-catalyzed azide-alkyne cycloaddition oncogenic-ras-harboring cancer cells genome-scale crispr perturbations undergo base-promoted hydrolysis remarkable proteome-wide selectivity crispr-cas9 essentiality screens azide-peg3-biotin conjugate mass spectrometry-based proteomics cysteine-targeting fumarate esters47 describe nitrile-oxide electrophiles pmc beta search chloroform/methanol/acetic acid/water masked nitrile-oxide electrophiles low proteome-wide selectivity lox-imvi cell-killing effects full-length western blots nitrile-oxide electrophiles generated anti-flag m2 agarose graphical abstract small-molecule thiol generates carboxylate-targeting isoxazolium48 probes gpx4-inhibiting chemotypes argues diverse gpx4-targeting chemotypes reactive nitrile-oxide electrophile gpx4_wt_flag-ptt5/spb2-ptt5 context-dependent binding contrasts harmony high-content imaging obvious protein-reactive group recombinant flag-gpx4wt protein purified wild-type gpx4 radical-trapping antioxidant ferrostatin-1 gpx4 active-site selenocysteine crispr library-infected cells α-nitroketoxime warheads exhibit /people/stuart-l-schreiber cell-active gpx4 inhibitors iron-dependent form chloroacetamide-based gpx4 inhibitors final protein-reactive metabolite selective gpx4-targeting warheads unique intact-cell dependence α-nitroketoxime initially yields intact-cell cetsa experiments intact-cell cetsa protocol glucosinolate engineering identifies α-nitroketoxime group highlighted ring-opening isomerization reaction gpx4-inhibiting tool compounds alumina promoted cyclization
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