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Citation
Poláková, M., Stanton, R., Wilson, I.B., Holková, I., Šesták, S., Machová, E., Jandová, Z., Kóňa, J. (2015). 'Click chemistry' synthesis of 1-(α-d-mannopyranosyl)-1,2,3-triazoles for inhibition of α-mannosidases.  Carbohydr. Res. 406(): 34--40.
FlyBase ID
FBrf0227645
Publication Type
Research paper
Abstract

Three new triazole conjugates derived from d-mannose were synthesized and assayed in in vitro assays to investigate their ability to inhibit α-mannosidase enzymes from the glycoside hydrolase (GH) families 38 and 47. The triazole conjugates were more selective for a GH47 α-mannosidase (Aspergillus saitoi α1,2-mannosidase), showing inhibition at the micromolar level (IC50 values of 50-250 μM), and less potent towards GH38 mannosidases (IC50 values in the range of 0.5-6 mM towards jack bean α-mannosidase or Drosophila melanogaster lysosomal and Golgi α-mannosidases). The highest selectivity ratio IC50(GH38)/IC50(GH47) of 100 was exhibited by the phenyltriazole conjugate. To understand structure-activity properties of synthesized compounds, 3-D complexes of inhibitors with α-mannosidases were built using molecular docking calculations.

PubMed ID
PubMed Central ID
PMC4382718 (PMC) (EuropePMC)
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Secondary IDs
    Language of Publication
    English
    Additional Languages of Abstract
    Parent Publication
    Publication Type
    Journal
    Abbreviation
    Carbohydr. Res.
    Title
    Carbohydrate Research
    Publication Year
    1965--
    ISBN/ISSN
    0008-6215
    Data From Reference
    Genes (2)