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Highly functionalized diaminocyclopentanes: A new route to potent and selective inhibitors of human O-GlcNAcase.
Weber, Patrick; Mészáros, Zuzana; Bojarová, Pavla; Ebner, Manuel; Fischer, Roland; Kren, Vladimír; Kulik, Natalia; Müller, Philipp; Vlachová, Miluse; Slámová, Kristýna; Stütz, Arnold E; Thonhofer, Martin; Torvisco, Ana; Wrodnigg, Tanja M; Wolfsgruber, Andreas.
Afiliação
  • Weber P; Glycogroup, Institute of Chemistry and Technology of Biobased Systems, Graz University of Technology, Stremayrgasse 9, A-8010 Graz, Austria. Electronic address: patrick.weber@tugraz.at.
  • Mészáros Z; Institute of Microbiology of the Czech Academy of Sciences, Vídenská 1083, CZ 14200, Prague 4, Czech Republic.
  • Bojarová P; Institute of Microbiology of the Czech Academy of Sciences, Vídenská 1083, CZ 14200, Prague 4, Czech Republic.
  • Ebner M; Glycogroup, Institute of Chemistry and Technology of Biobased Systems, Graz University of Technology, Stremayrgasse 9, A-8010 Graz, Austria.
  • Fischer R; Institute of Inorganic Chemistry, Graz University of Technology, Stremayrgasse 9, A-8010 Graz, Austria.
  • Kren V; Institute of Microbiology of the Czech Academy of Sciences, Vídenská 1083, CZ 14200, Prague 4, Czech Republic.
  • Kulik N; Institute of Microbiology of the Czech Academy of Sciences, Vídenská 1083, CZ 14200, Prague 4, Czech Republic.
  • Müller P; Institute of Inorganic Chemistry, Graz University of Technology, Stremayrgasse 9, A-8010 Graz, Austria.
  • Vlachová M; Institute of Microbiology of the Czech Academy of Sciences, Vídenská 1083, CZ 14200, Prague 4, Czech Republic.
  • Slámová K; Institute of Microbiology of the Czech Academy of Sciences, Vídenská 1083, CZ 14200, Prague 4, Czech Republic.
  • Stütz AE; Glycogroup, Institute of Chemistry and Technology of Biobased Systems, Graz University of Technology, Stremayrgasse 9, A-8010 Graz, Austria.
  • Thonhofer M; Glycogroup, Institute of Chemistry and Technology of Biobased Systems, Graz University of Technology, Stremayrgasse 9, A-8010 Graz, Austria.
  • Torvisco A; Institute of Inorganic Chemistry, Graz University of Technology, Stremayrgasse 9, A-8010 Graz, Austria.
  • Wrodnigg TM; Glycogroup, Institute of Chemistry and Technology of Biobased Systems, Graz University of Technology, Stremayrgasse 9, A-8010 Graz, Austria.
  • Wolfsgruber A; Glycogroup, Institute of Chemistry and Technology of Biobased Systems, Graz University of Technology, Stremayrgasse 9, A-8010 Graz, Austria.
Bioorg Chem ; 140: 106819, 2023 11.
Article em En | MEDLINE | ID: mdl-37666109
ABSTRACT
A new class of compounds inhibiting de-O-glycosylation of proteins has been identified. Highly substituted diaminocyclopentanes are impressively selective reversible non-transition state O-ß-N-acetyl-d-glucosaminidase (O-GlcNAcase) inhibitors. The ease of preparative access and remarkable biological activities provide highly viable leads for the development of anti-tau-phosphorylation agents with a view to eventually ameliorating Alzheimer's disease.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Beta-N-Acetil-Hexosaminidases / Doença de Alzheimer Limite: Humans Idioma: En Ano de publicação: 2023 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Beta-N-Acetil-Hexosaminidases / Doença de Alzheimer Limite: Humans Idioma: En Ano de publicação: 2023 Tipo de documento: Article