ArticleFEBS letters2010
Screening-based discovery of drug-like O-GlcNAcase inhibitor scaffolds.
Article in FEBS letters, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
What it found
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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
16 citing papers in PubMed, 32 citations in OpenAlex.
- Small molecule splicing modulators that disrupt O-GlcNAc homeostasis.Nature communications · 2026Article
- Recent Progress of Small-molecule Inhibitors of O-GlcNAcase for Alzheimer's Disease.Mini reviews in medicinal chemistry · 2025Review
- O-GlcNAcylation as a Therapeutic Target for Alzheimer's Disease.Neuromolecular medicine · 2020Review
- Plant chemical genetics reveals colistin sulphate as a SA and NPR1-independent PR1 inducer functioning via a p38-like kinase pathway.Scientific reports · 2019Article
- O-GlcNAcase Fragment Discovery with Fluorescence Polarimetry.ACS chemical biology · 2018Article
- Finding the molecular scaffold of nuclear receptor inhibitors through high-throughput screening based on proteochemometric modelling.Journal of cheminformatics · 2018Article
- Inhibition ofMolecular cancer therapeutics · 2018Article
- Hyper-O-GlcNAcylation induces cisplatin resistance via regulation of p53 and c-Myc in human lung carcinoma.Scientific reports · 2017Article
- The Early Metazoan Trichoplax adhaerens Possesses a Functional O-GlcNAc System.The Journal of biological chemistry · 2015Article
- Discovery of selective small-molecule activators of a bacterial glycoside hydrolase.Angewandte Chemie (International ed. in English) · 2014Article
- Development of Unsymmetrical Dyads As Potent Noncarbohydrate-Based Inhibitors against Human β-N-Acetyl-d-hexosaminidase.ACS medicinal chemistry letters · 2013Article
- Developing inhibitors of glycan processing enzymes as tools for enabling glycobiology.Nature chemical biology · 2012Review
- The roles of O-linked β-N-acetylglucosamine in cardiovascular physiology and disease.American journal of physiology. Heart and circulatory physiology · 2012Review
- Detection and analysis of proteins modified by O-linked N-acetylglucosamine.Current protocols in protein science · 2011Article
- O-GlcNAc signalling: implications for cancer cell biology.Nature reviews. Cancer · 2011Review
- Detection and analysis of proteins modified by O-linked N-acetylglucosamine.Current protocols in molecular biology · 2011Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
O-GlcNAcylation is an essential posttranslational modification in metazoa. Modulation of O-GlcNAc levels with small molecule inhibitors of O-GlcNAc hydrolase (OGA) is a useful strategy to probe the role of this modification in a range of cellular processes. Here we report the discovery of novel, low molecular weight and drug-like O-GlcNAcase inhibitor scaffolds by high-throughput screening. Kinetic and X-ray crystallographic analyses of the binding modes with human/bacterial O-GlcNAcases identify some of these as competitive inhibitors. Comparative kinetic experiments with the mechanistically related human lysosomal hexosaminidases reveal that three of the inhibitor scaffolds show selectivity towards human OGA. These scaffolds provide attractive starting points for the development of non-carbohydrate, drug-like OGA inhibitors.
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Registered trials
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.