Guo, Tianlin and Dätwyler, Philipp and Demina, Ekaterina and Richards, Michele R. and Ge, Peng and Zou, Chunxia and Zheng, Ruixiang and Fougerat, Anne and Pshezhetsky, Alexey V. and Ernst, Beat and Cairo, Christopher W.. (2018) Selective Inhibitors of Human Neuraminidase 3. Journal of medicinal chemistry, 61 (5). pp. 1990-2008.
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Official URL: https://edoc.unibas.ch/68233/
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Abstract
Human neuraminidases (NEU) are associated with human diseases including cancer, atherosclerosis, and diabetes. To obtain small molecule inhibitors as research tools for the study of their biological functions, we designed a library of 2-deoxy-2,3-didehydro- N-acetylneuraminic acid (DANA) analogues with modifications at C4 and C9 positions. This library allowed us to discover selective inhibitors targeting the human NEU3 isoenzyme. Our most selective inhibitor for NEU3 has a K; i; of 320 ± 40 nM and a 15-fold selectivity over other human neuraminidase isoenzymes. This inhibitor blocks glycolipid processing by NEU3 in vitro. To improve their pharmacokinetic properties, various esters of the best inhibitors were synthesized and evaluated. Finally, we confirmed that our best compounds exhibited selective inhibition of NEU orthologues from murine brain.
| Faculties and Departments: | 05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Ehemalige Einheiten Pharmazie > Molekulare Pharmazie (Ernst) |
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| UniBasel Contributors: | Ernst, Beat and Dätwyler, Philipp |
| Item Type: | Article, refereed |
| Article Subtype: | Research Article |
| ISSN: | 1520-4804 |
| Note: | Publication type according to Uni Basel Research Database: Journal article |
| Identification Number: |
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| Last Modified: | 15 Apr 2020 16:00 |
| Deposited On: | 15 Apr 2020 16:00 |
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