ArticleNature communications2019
Structure and inhibition mechanism of the catalytic domain of human squalene epoxidase.
Article in Nature communications, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 81 papers, 1 of them a synthesis that pooled it.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
81 citing papers in PubMed, 1 synthesis or guideline pooled it, 77 citations in OpenAlex.
- Squalene Epoxidase: Its Regulations and Links with Cancers.International journal of molecular sciences · 2024Pooled it
- Unveiling the Mechanisms of Ozone-Induced Male Reproductive Toxicity: Insights from Testicular Proteomics and CTD Database.Environment & health (Washington, D.C.) · 2026Article
- Insights into Enzymes Involved in the Biosynthesis of Protopanaxadiol-Type Ginsenosides inACS omega · 2026Review
- Deciphering the genomic landscape ofMicrobial genomics · 2026Article
- Dual PCR-Sanger Sequencing Assay for Simultaneous sqle-Based Identification and Resistance Detection in Trichophyton Species.Emerging infectious diseases · 2026Article
- Size-Resolved Lipoprotein Fatty Acid Content as a Novel Nuclear Magnetic Resonance-Derived Trait Specifically Associates with Genetic Variants That Control Fatty Acid Metabolism.Journal of proteome research · 2026Article
- Synthetic Sinapates: Antifungal, Molecular Docking, and ADMET Studies.Chemistry & biodiversity · 2026Article
- Low temperature rather than hypoxia drives cholesterol synthesis and oxygen consumption in plateau zokors.iScience · 2026Article
- Squalene epoxidase promotes paraquat-induced pulmonary toxicity through endoplasmic reticulum-mediated ferroptosis.Journal of advanced research · 2026Article
- Squalene Epoxidase: A Key Enzymatic Component in the Triterpenoid Biosynthesis Pathway.Applied biochemistry and biotechnology · 2026Review
- Network and molecular insights into the antidiabetic potential of squalene in alloxan-induced diabetes.Scientific reports · 2026Article
- Review
- Lipid metabolism dysregulation in solar lentigo: a multi-system-level analysis reveals membrane instability and energy homeostasis disruption.Frontiers in cell and developmental biology · 2026Article
- In vitro and in vivo efficacy of the antimycobacterial molecule SQ109 against the human pathogenic fungus, Cryptococcus neoformans.PLoS neglected tropical diseases · 2025Article
- Mechanistic Insights into Polyphenols-mediated Squalene Epoxidase Inhibition: Computational Models and Experimental Validation for Targeting Cholesterol Biosynthesis.Cell biochemistry and biophysics · 2025Article
- Ferroptosis in Diabetic Cardiomyopathy and Atherosclerosis: Mechanisms and Clinical Prospects.International journal of molecular sciences · 2025Review
- Identification and validation of SQLE in steroid-induced osteonecrosis of the femoral head: a bioinformatics and experimental study.Journal of orthopaedic surgery and research · 2025Article
- Mechanism-based inhibition of squalene epoxidase by phenothiazines for lipid metabolism disruption using repurposed antipsychotic drugs.Scientific reports · 2025Article
- Age-Associated Proteomic Changes in Human Spermatozoa.International journal of molecular sciences · 2025Article
- Structural Basis of Sequential Enantioselective Epoxidation by a Flavin-Dependent Monooxygenase in Lasalocid A Biosynthesis.Angewandte Chemie (International ed. in English) · 2025Article
21 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
17 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Squalene epoxidase (SQLE), also known as squalene monooxygenase, catalyzes the stereospecific conversion of squalene to 2,3(S)-oxidosqualene, a key step in cholesterol biosynthesis. SQLE inhibition is targeted for the treatment of hypercholesteremia, cancer, and fungal infections. However, lack of structure-function understanding has hindered further progression of its inhibitors. We have determined the first three-dimensional high-resolution crystal structures of human SQLE catalytic domain with small molecule inhibitors (2.3 Å and 2.5 Å). Comparison with its unliganded state (3.0 Å) reveals conformational rearrangements upon inhibitor binding, thus allowing deeper interpretation of known structure-activity relationships. We use the human SQLE structure to further understand the specificity of terbinafine, an approved agent targeting fungal SQLE, and to provide the structural insights into terbinafine-resistant mutants encountered in the clinic. Collectively, these findings elucidate the structural basis for the specificity of the epoxidation reaction catalyzed by SQLE and enable further rational development of next-generation inhibitors.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.