ArticleActa crystallographica. Section D, Structural biology2021
Crystal structures of the selenoprotein glutathione peroxidase 4 in its apo form and in complex with the covalently bound inhibitor ML162.
Article in Acta crystallographica. Section D, Structural biology, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 50 papers.
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Who cites it
50 citing papers in PubMed, 108 citations in OpenAlex.
- Degrading GPX4 via Biomimetic Nanoparticle-Mediated In Situ Synthesis of Deep-Learning-Designed Binder-Degron Chimeras for Prostate Cancer Therapy.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- A Crystalline and Thermally Stable Selenocysteine Selenenic Acid.Angewandte Chemie (International ed. in English) · 2026Article
- Article
- Design, Synthesis, and Protective Activity against Doxorubicin-Induced Cardiotoxicity of Novel Water-Soluble Small-Molecule GPx Mimics.ACS medicinal chemistry letters · 2026Article
- Plumbagin Induces Ferroptosis in Nonfunctioning Pituitary Adenomas via Nrf2/FTH1-Dependent Ferritinophagy.Drug design, development and therapy · 2026Article
- Targeting ZNRF2-mediated SLC3A2 plasma membrane translocation enhances ferroptosis in lung adenocarcinoma.Oncogene · 2025Article
- Targeted ferroptosis induction enhances chemotherapy efficacy in chemoresistant neuroblastoma.NPJ precision oncology · 2025Article
- Ferroptosis in Cancer and Inflammatory Diseases: Mechanisms and Therapeutic Implications.MedComm · 2025Review
- Prospects for ferroptosis therapies in cancer.Nature cancer · 2025Review
- Discovery and validation of indole nitroolefins as novel covalent GPX4 inhibitors for inducing ferroptosis in urological cancers.Chinese journal of cancer research = Chung-kuo yen cheng yen chiu · 2025Article
- Noscapine derivative 428 suppresses ferroptosis through targeting GPX4.Redox biology · 2025Article
- Protein covariation networks for elucidating ferroptosis inducer mechanisms and potential synergistic drug targets.Communications biology · 2025Article
- Identification of a Selective Anticancer Agent from a Collection of Complex-And-Diverse Compounds Synthesized from Stevioside.Journal of the American Chemical Society · 2025Article
- USP5 Suppresses Ferroptosis in Bladder Cancer Through Stabilization of GPX4.Current issues in molecular biology · 2025Article
- Iron homeostasis and ferroptosis in muscle diseases and disorders: mechanisms and therapeutic prospects.Bone research · 2025Review
- GPX modulation promotes regenerative axonal fusion and functional recovery after injury through PSR-1 condensation.Nature communications · 2025Article
- Recent Progress of Glutathione Peroxidase 4 Inhibitors in Cancer Therapy.Mini reviews in medicinal chemistry · 2025Review
- Iron Overloading Potentiates the Antitumor Activity of 5-Fluorouracil by Promoting Apoptosis and Ferroptosis in Colorectal Cancer Cells.Cell biochemistry and biophysics · 2024Article
- Ferroptosis in health and disease.Redox biology · 2024Review
- Oxidative cell death in cancer: mechanisms and therapeutic opportunities.Cell death & disease · 2024Review
Corrections and comments
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Authors and funding
12 authors at 2 institutions in 2 countries.
Funding
Abstract
Wild-type human glutathione peroxidase 4 (GPX4) was co-expressed with SBP2 (selenocysteine insertion sequence-binding protein 2) in human HEK cells to achieve efficient production of this selenocysteine-containing enzyme on a preparative scale for structural biology. The protein was purified and crystallized, and the crystal structure of the wild-type form of GPX4 was determined at 1.0 Å resolution. The overall fold and the active site are conserved compared with previously determined crystal structures of mutated forms of GPX4. A mass-spectrometry-based approach was developed to monitor the reaction of the active-site selenocysteine Sec46 with covalent inhibitors. This, together with the introduction of a surface mutant (Cys66Ser), enabled the crystal structure determination of GPX4 in complex with the covalent inhibitor ML162 [(S)-enantiomer]. The mass-spectrometry-based approach described here opens the path to further co-complex crystal structures of this potential cancer drug target in complex with covalent inhibitors.
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