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Synthesis of modified D-mannose core derivatives and their impact on GH38 α-mannosidases
- Poláková, Monika, Horák, Radim, Šesták, Sergej, Holková, Ivana
- Carbohydrate research 2016 v.428 pp. 62-71
- Canavalia ensiformis, Drosophila melanogaster, alpha-mannosidase, humans, inhibitory concentration 50, mannose, triazoles
- Nine new compounds having five- and modified six-member carbohydrate core derived from D-lyxose or D-mannose, and non-hydrolysable aglycones (benzylsulfonyl or aryl(alkyl)triazolyl) were synthesised to investigate their ability to inhibit the recombinant Drosophila melanogaster homologs of two human GH38 family enzymes: Golgi mannosidase II (dGMIIb) and lysosomal mannosidase (dLMII).Two compounds were weak selective dGMIIb inhibitors showing IC50 at mM level. Moreover, it was found that another GH38 enzyme, commercial jack bean α-mannosidase, was inhibited by triazole conjugates regardless of the carbohydrate core while the corresponding sulfones were inactive.