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Literature summary extracted from

  • Kumar, N.S.; Kuntz, D.A.; Wen, X.; Pinto, B.M.; Rose, D.R.
    Binding of sulfonium-ion analogues of di-epi-swainsonine and 8-epi-lentiginosine to Drosophila Golgi alpha-mannosidase II: The role of water in inhibitor binding (2008), Proteins, 71, 1484-1496.
    View publication on PubMed

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
3.2.1.114 by hanging-drop vapor diffusion method, GMII in complex with inhibitors di-epi-swainsonine and 8-epi-lentiginosine, both adopt a 3C6/E7 conformation, water molecule substructure in the active site plays a significant role in dictating inhibitory activity Drosophila melanogaster

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.2.1.114 (1R,2S,8aS)-1,2-dihydroxyoctahydrothieno[1,2-a]thiopyranium chloride good inhibitor, lacks a hydroxyl group at C-5, more than 140fold better inhibitor of GMII than di-epi-swainsonine Drosophila melanogaster
3.2.1.114 8-epi-lentiginosine
-
 Drosophila melanogaster
3.2.1.114 di-epi-swainsonine weak inhibitor Drosophila melanogaster
3.2.1.114 Mannostatin A
-
 Drosophila melanogaster
3.2.1.114 swainsonine
-
 Drosophila melanogaster

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
3.2.1.114 Zn2+ di-epi-swainsonine has only a single hydroxyl group at C-8 interacting with the zinc ion of the enzyme Drosophila melanogaster

Organism

EC Number Organism UniProt Comment Textmining
3.2.1.114 Drosophila melanogaster Q24451
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.2.1.114
-
 Drosophila melanogaster

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.2.1.114 4-nitrophenyl alpha-D-mannoside + H2O
-
 Drosophila melanogaster 4-nitrophenol + alpha-D-mannose
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.2.1.114 GmII
-
 Drosophila melanogaster
3.2.1.114 Golgi alpha-mannosidase II
-
 Drosophila melanogaster

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.2.1.114 0.014
-
-
 Drosophila melanogaster 8-epi-lentiginosine
3.2.1.114 2
-
-
 Drosophila melanogaster di-epi-swainsonine