ArticleACS medicinal chemistry letters2013
Identification of Selective Nanomolar Inhibitors of the Human Neuraminidase, NEU4.
Article in ACS medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 51 citations in OpenAlex.
- Sialidases as Potential Therapeutic Targets for Treatment of a Number of Human Diseases.International journal of molecular sciences · 2025Review
- Improved C5-Amide Bioisosteres for Human Neuraminidase 1 Inhibitors Based on 2-Deoxy-2,3-Didehydro-N-Acetyl Neuraminic Acid.ChemMedChem · 2025Article
- Discovering Influenza Virus Neuraminidase Inhibitors via Computational and Experimental Studies.ACS omega · 2024Article
- Synthetic Sialosides Terminated with 8-N-Substituted Sialic Acid as Selective Substrates for Sialidases from Bacteria and Influenza Viruses.Angewandte Chemie (International ed. in English) · 2024Article
- MedChemExpress compounds prevent neuraminidase N1RSC advances · 2024Article
- The role of sialidase Neu1 in respiratory diseases.Respiratory research · 2024Review
- Sialidase Inhibitors with Different Mechanisms.Journal of medicinal chemistry · 2022Review
- Azido Groups Hamper Glycan Acceptance by Carbohydrate Processing Enzymes.ACS central science · 2022Article
- The Janus-like role of neuraminidase isoenzymes in inflammation.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2022Article
- Inhibitors of Human Neuraminidase Enzymes Block TransmigrationFrontiers in molecular biosciences · 2022Article
- The Function of Sialidase Revealed by Sialidase Activity Imaging Probe.International journal of molecular sciences · 2021Review
- Neuraminidases 1 and 3 Trigger Atherosclerosis by Desialylating Low-Density Lipoproteins and Increasing Their Uptake by Macrophages.Journal of the American Heart Association · 2021Article
- Sialidase and Sialyltransferase Inhibitors: Targeting Pathogenicity and Disease.Frontiers in molecular biosciences · 2021Review
- The sialidase inhibitor 2,3-dehydro-2-deoxy-N-acetylneuraminic acid is a glucose-dependent potentiator of insulin secretion.Scientific reports · 2020Article
- Triazole-linked transition state analogs as selective inhibitors against V. cholerae sialidase.Bioorganic & medicinal chemistry · 2018Article
- Keeping it trim: roles of neuraminidases in CNS function.Glycoconjugate journal · 2018Review
- Sialidase-catalyzed one-pot multienzyme (OPME) synthesis of sialidase transition-state analogue inhibitors.ACS catalysis · 2018Article
- TheFrontiers in microbiology · 2017Article
- The NEU1-selective sialidase inhibitor, C9-butyl-amide-DANA, blocks sialidase activity and NEU1-mediated bioactivities in human lung in vitro and murine lung in vivo.Glycobiology · 2016Article
- Article
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Authors and funding
5 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The human neuraminidase enzymes (hNEU) play important roles in human physiology and pathology. The lack of potent and selective inhibitors toward these enzymes has limited our understanding of their function and the development of therapeutic applications. Here we report the evaluation of a panel of compounds against the four human neuraminidase isoenzymes. Among the compounds tested, we identified the first selective, nanomolar inhibitors of the human neuraminidase 4 enzyme (NEU4). The most potent NEU4 inhibitor (5-acetamido-9-[4-hydroxymethyl[1,2,3]triazol-1-yl]-2,3,5,9-tetradeoxy-d-glycero-d-galacto-2-nonulopyranosonic acid) was found to have an inhibitory constant (K i ) of 30 ± 19 nM and was 500-fold selective for its target over the other hNEU isoenzymes tested in vitro (NEU1, NEU2, and NEU3). This is the first report of any inhibitor of hNEU with nanomolar potency, and this confirms that the 2,3-didehydro-2-deoxy-N-acetylneuraminic acid (DANA) scaffold can be exploited to develop new, potent, and selective inhibitors that target this important family of human enzymes.
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Registered trials
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