WebApr 11, 2024 · The inhibition of ALDH3a2 induces ferroptosis and exerts synergistic anti-leukemia effects with GPX4 inhibition or standard chemotherapy with cytarabine plus … WebApr 12, 2024 · Similarly, the protein expression of GPX4 (Figure 3E,F) and xCT (Figure 3E) were decreased in bEnd.3 cells with 12 h incubation of hypoxia. Taken together, ferroptosis of BMECs contributed to the BBB disruption under short-term hypoxia. The ferroptosis inhibitor Fer-1 alleviated hypoxia-induced BBB disruption
Identification of a small molecule as inducer of ferroptosis and ...
WebApr 7, 2024 · A decrease in the expression of the ferroptosis inhibition genes (GPX4, GSS, GCLC, SLCA11, SLC3A2) and an increase in ACLS4 was observed in the CD274_high … A chief drawback of chloroacetamide GPX4 inhibitors is their high chemical reactivity, which imparts them with relatively low proteome-wide selectivity. To test whether ML210 may act in a more selective manner, we performed cellular proteome reactivity profiling experiments using the ML210, RSL3 … See more To identify small-molecule GPX4 inhibitors that do not contain a reactive alkyl chloride warhead, we focused our attention on the nitroisoxazole … See more To understand how ML210 covalently modifies GPX4 without a chloroacetamide warhead, we developed an intact protein mass spectrometry … See more The +434 Da mass of the ML210-derived GPX4 adduct suggests that the final protein-reactive metabolite of ML210 is related to JKE-1674 through the loss of water. In cells, ML210 and JKE-1674 react with cysteine and … See more To investigate how ML210 may give rise in cells to a GPX4-targeting metabolite, we focused our attention on the nitroisoxazole group, which … See more inboard scooter
Discovery of a Potent Chloroacetamide GPX4 Inhibitor …
WebJan 7, 2024 · GPX4 inhibitor–mediated cell death was accompanied by accumulation of lipid hydroperoxides, suggesting ferroptotic cell death, and could be rescued by the lipophilic antioxidants ferrostatin-1 or liproxstatin-1, further confirming that … WebAug 9, 2024 · GPX4 is the only cellular enzyme that specifically reduces phospholipid hydroperoxides to lipid alcohols using GSH as a co-factor 4, and inhibiting the cyst (e)ine/GSH/GPX4 axis induces the... WebGPX4 is a key regulator of ferroptosis that inhibits ferroptotic cell death by preventing iron-dependent accumulation of toxic phospholipid hydroperoxide species.2Cancer cells in a high-mesenchymal state, and those that persist after treatment, are dependent on GPX4 and are particularly susceptible to ferroptosis.9,10Inhibition of GPX4 by ML-210 … in and out burger t shirt