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Literature summary for 3.2.1.114 extracted from

  • Englebienne, P.; Fiaux, H.; Kuntz, D.A.; Corbeil, C.R.; Gerber-Lemaire, S.; Rose, D.R.; Moitessier, N.
    Evaluation of docking programs for predicting binding of Golgi alpha-mannosidase II inhibitors: a comparison with crystallography (2007), Proteins, 69, 160-176.
    View publication on PubMed
Search for more literature for 3.2.1.114

Application

Application Comment Organism
medicine promising target for drug development in anti-tumor therapies, ability of seven available docking programs to predict the binding mode and binding affinity of alpha-mannosidase II inhibitors Drosophila melanogaster

Crystallization (Commentary)

Crystallization (Comment) Organism
GMII complexed with inhibitors (2R,3R,4S)-2-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidine-3,4-diol, (2R,3R,4S)-2-([[(1S)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidine-3,4-diol, and (2R,3R,4S,5R)-2-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)-5-methylpyrrolidine-3,4-diol, to 1.30-1.45 A resolution Drosophila melanogaster

Inhibitors

Inhibitors Comment Organism Structure
(1S,2R,6R,7R,8S,8aS)-octahydroindolizine-1,2,6,7,8-pentol most active Drosophila melanogaster
(2R,3R,4R,5R)-2-(hydroxymethyl)piperidine-3,4,5-triol
-
 Drosophila melanogaster
(2R,3R,4R,5R)-5-amino-2-(hydroxymethyl)piperidine-3,4-diol
-
 Drosophila melanogaster
(2R,3R,4S)-2-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidine-3,4-diol
-
 Drosophila melanogaster
(2R,3R,4S)-2-([[(1S)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidine-3,4-diol
-
 Drosophila melanogaster
(2R,3R,4S,5R)-2-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)-5-methylpyrrolidine-3,4-diol
-
 Drosophila melanogaster
(2R,3R,4S,5S)-6-amino-2-(hydroxymethyl)-2,3,4,5-tetrahydropyridine-3,4,5-triol
-
 Drosophila melanogaster
(2R,3S,4R)-2-[(1R)-1-hydroxyethyl]pyrrolidine-3,4-diol most active Drosophila melanogaster
(2R,3S,4S)-1-[(2S,3S)-2,4-dihydroxy-3-(sulfooxy)butyl]-3,4-dihydroxy-2-(hydroxymethyl)tetrahydrothiophenium
-
 Drosophila melanogaster
(3R,4R)-4-aminopyrrolidin-3-ol
-
 Drosophila melanogaster
(5R,6R,7S,8R)-5-methyl-1,5,6,7,8,8a-hexahydrotetrazolo[1,5-a]pyridine-6,7,8-triol
-
 Drosophila melanogaster
(5R,6R,7S,8S)-5-(hydroxymethyl)-1,5,6,7,8,8a-hexahydroimidazo[1,2-a]pyridine-6,7,8-triol
-
 Drosophila melanogaster
5-thio-alpha-D-mannopyranosylamine
-
 Drosophila melanogaster
kifunensine
-
 Drosophila melanogaster
N-[(R)-amino(phenyl)methyl]-5-thio-alpha-D-mannopyranosylamine
-
 Drosophila melanogaster
salacinol
-
 Drosophila melanogaster
swainsonine most active Drosophila melanogaster

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+ is involved in the catalytic activity of the enzyme and in the strong binding of inhibitors Drosophila melanogaster

Organism

Organism UniProt Comment Textmining
Drosophila melanogaster Q24451
-
-

Synonyms

Synonyms Comment Organism
GmII
-
 Drosophila melanogaster
Golgi alpha-mannosidase II
-
 Drosophila melanogaster

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000017
-
-
 Drosophila melanogaster swainsonine
0.72
-
-
 Drosophila melanogaster (2R,3R,4S)-2-([[(1S)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidine-3,4-diol
0.8
-
-
 Drosophila melanogaster (2R,3R,4S)-2-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidine-3,4-diol
1
-
-
 Drosophila melanogaster (2R,3R,4S,5R)-2-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)-5-methylpyrrolidine-3,4-diol