Number of the records: 1
Diaminocyclopentane-derived O-GlcNAcase inhibitors for combating tau hyperphosphorylation in Alzheimer's disease
- 1.
SYSNO ASEP 0560090 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Diaminocyclopentane-derived O-GlcNAcase inhibitors for combating tau hyperphosphorylation in Alzheimer's disease Author(s) Weber, P. (AT)
Mészáros, Zuzana (MBU-M)
Jagecic, D. (HR)
Hribljan, V. (HR)
Mitrečic, D. (HR)
Bojarová, Pavla (MBU-M) ORCID
Slámová, Kristýna (MBU-M) RID, ORCID
Vrba, J. (CZ)
Kulik, Natalia (MBU-M) ORCID
Křen, Vladimír (MBU-M) RID, ORCID
Stuetz, A. E. (AT)Source Title Chemical Communications. - : Royal Society of Chemistry - ISSN 1359-7345
Roč. 58, č. 63 (2022), s. 8838-8841Number of pages 4 s. Language eng - English Country GB - United Kingdom Keywords primary human hepatocyteskinetic ; kinetic-analysis ; enzyme level ; hepg2 cells ; hexosaminidase ; mechanisms ; induction Subject RIV CE - Biochemistry OECD category Biochemistry and molecular biology R&D Projects GF21-01948L GA ČR - Czech Science Foundation (CSF) Method of publishing Limited access Institutional support MBU-M - RVO:61388971 UT WOS 000826603200001 EID SCOPUS 85134978123 DOI 10.1039/d2cc02712g Annotation We developed potent and selective aminocyclopentane-derived inhibitors of human O-N-acetyl-beta-d-glucosaminidase (OGA) implicated in Alzheimer's disease. For example compound 13 was a nanomolar OGA inhibitor with 92 000-fold selectivity over human HexB. It was non-toxic and increased protein O-GlcNAcylation in the culture of murine neural cells, showing new alternatives in the treatment of tauopathies. Workplace Institute of Microbiology Contact Eliška Spurná, eliska.spurna@biomed.cas.cz, Tel.: 241 062 231 Year of Publishing 2023 Electronic address https://pubs.rsc.org/en/content/articlelanding/2022/CC/D2CC02712G
Number of the records: 1