Gewählte Publikation:
SHR
Neuro
Krebs
Kardio
Lipid
Stoffw
Microb
Thonhofer, M; Weber, P; Santana, AG; Fischer, R; Pabst, BM; Paschke, E; Schalli, M; Stütz, AE; Tschernutter, M; Windischhofer, W; Withers, SG.
Synthesis of C-5a-chain extended derivatives of 4-epi-isofagomine: Powerful β-galactosidase inhibitors and low concentration activators of GM1-gangliosidosis-related human lysosomal β-galactosidase.
Bioorg Med Chem Lett. 2016; 26(5):1438-1442
Doi: 10.1016/j.bmcl.2016.01.059
Web of Science
PubMed
FullText
FullText_MUG
- Co-Autor*innen der Med Uni Graz
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Pabst Bettina
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Paschke Eduard
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Schalli Michael
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Tschernutter Marion
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Windischhofer Werner
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- Abstract:
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From an easily available partially protected formal derivative of 1-deoxymannojirimycin, by hydroxymethyl chain-branching and further elaboration, lipophilic analogs of the powerful β-d-galactosidase inhibitor 4-epi-isofagomine have become available. New compounds exhibit improved inhibitory activities comparable to benchmark compound NOEV (N-octyl-epi-valienamine) and may serve as leads towards improved and more selective pharmacological chaperones for GM1-gangliosidosis.
Copyright © 2016 Elsevier Ltd. All rights reserved.
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Dose-Response Relationship, Drug -
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Enzyme Inhibitors - chemical synthesis
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Enzyme Inhibitors - chemistry
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Enzyme Inhibitors - pharmacology
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Gangliosidosis, GM1 - enzymology
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Gangliosidosis, GM1 - pathology
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Humans -
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Imino Pyranoses - chemical synthesis
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Imino Pyranoses - chemistry
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Imino Pyranoses - pharmacology
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Lysosomes - drug effects
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Lysosomes - enzymology
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Models, Molecular -
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Molecular Structure -
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Structure-Activity Relationship -
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beta-Galactosidase - antagonists & inhibitors
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beta-Galactosidase - metabolism
- Find related publications in this database (Keywords)
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Iminoalditol
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4-epi-Isofagomine
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Galactosidase inhibitor
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Pharmacological chaperone
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G(M1)-gangliosidosis