ArticleChemistry & biology2010
Cell-penetrant, nanomolar O-GlcNAcase inhibitors selective against lysosomal hexosaminidases.
Article in Chemistry & biology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
28 citing papers in PubMed, 58 citations in OpenAlex.
- O-GlcNAcylation: the metabolic-immune translator in tumor evolution and treatment.Molecular medicine (Cambridge, Mass.) · 2026Review
- Protein O-GlcNAcylation in Health and Diseases.MedComm · 2025Review
- Recent Progress of Small-molecule Inhibitors of O-GlcNAcase for Alzheimer's Disease.Mini reviews in medicinal chemistry · 2025Review
- Article
- Advances in chemical probing of proteinChemical Society reviews · 2021Review
- Molecular Interrogation to Crack the Case of O-GlcNAc.Chemistry (Weinheim an der Bergstrasse, Germany) · 2020Review
- Loss of CRMP2 O-GlcNAcylation leads to reduced novel object recognition performance in mice.Open biology · 2019Article
- Genetic recoding to dissect the roles of site-specific protein O-GlcNAcylation.Nature structural & molecular biology · 2019Article
- Review
- Computational Studies on the Potency and Selectivity of PUGNAc Derivatives Against GH3, GH20, and GH84 β-N-acetyl-D-hexosaminidases.Frontiers in chemistry · 2019Article
- O-GlcNAcase Fragment Discovery with Fluorescence Polarimetry.ACS chemical biology · 2018Article
- Potent GH20 N-Acetyl-β-d-hexosaminidase Inhibitors: N-Substituted 3-acetamido-4-amino-5-hydroxymethyl-cyclopentanediols.Molecules (Basel, Switzerland) · 2018Article
- Deciphering the Functions of Protein O-GlcNAcylation with Chemistry.ACS chemical biology · 2017Review
- Dissecting PUGNAc-mediated inhibition of the pro-survival action of insulin.Glycobiology · 2016Article
- Analysis of transition state mimicry by tight binding aminothiazoline inhibitors provides insight into catalysis by humanChemical science · 2016Article
- Glucose and glutamine fuel protein O-GlcNAcylation to control T cell self-renewal and malignancy.Nature immunology · 2016Article
- Mechanism of Human Nucleocytoplasmic Hexosaminidase D.Biochemistry · 2016Article
- Evidence for a Functional O-Linked N-Acetylglucosamine (O-GlcNAc) System in the Thermophilic Bacterium Thermobaculum terrenum.The Journal of biological chemistry · 2015Article
- O-GlcNAcase: promiscuous hexosaminidase or key regulator of O-GlcNAc signaling?The Journal of biological chemistry · 2014Review
- O-GlcNAc and the cardiovascular system.Pharmacology & therapeutics · 2014Review
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
Posttranslational modification of metazoan nucleocytoplasmic proteins with N-acetylglucosamine (O-GlcNAc) is essential, dynamic, and inducible and can compete with protein phosphorylation in signal transduction. Inhibitors of O-GlcNAcase, the enzyme removing O-GlcNAc, are useful tools for studying the role of O-GlcNAc in a range of cellular processes. We report the discovery of nanomolar OGA inhibitors that are up to 900,000-fold selective over the related lysosomal hexosaminidases. When applied at nanomolar concentrations on live cells, these cell-penetrant molecules shift the O-GlcNAc equilibrium toward hyper-O-GlcNAcylation with EC₅₀ values down to 3 nM and are thus invaluable tools for the study of O-GlcNAc cell biology.
Indexed as
Identifiers
What OpenQuestion holds
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.