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Literature summary for 3.2.1.24 extracted from

  • Fiaux, H.; Kuntz, D.A.; Hoffman, D.; Janzer, R.C.; Gerber-Lemaire, S.; Rose, D.R.; Juillerat-Jeanneret, L.
    Functionalized pyrrolidine inhibitors of human type II alpha-mannosidases as anti-cancer agents: optimizing the fit to the active site (2008), Bioorg. Med. Chem., 16, 7337-7346.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(1S,2R,8R,8aR)-octahydroindolizine-1,2,8-triol
-
Canavalia sp.
(1S,2R,8R,8aR)-octahydroindolizine-1,2,8-triol
-
Homo sapiens
(2R,3R,4S)-2-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidine-3,4-diol
-
Canavalia sp.
(2R,3R,4S)-2-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidine-3,4-diol
-
Homo sapiens
(3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)-1-methylpyrrolidin-2-one
-
Canavalia sp.
(3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)-1-methylpyrrolidin-2-one
-
Homo sapiens
(3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidin-2-one
-
Canavalia sp.
(3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidin-2-one
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.55
-
4-methylumbelliferyl-alpha-D-mannopyranoside pH 5.0, 37°C, HCEC cell layer Homo sapiens
0.65
-
4-methylumbelliferyl-alpha-D-mannopyranoside pH 5.0, 37°C, LNZ-308 cell layer Homo sapiens
1.065
-
4-methylumbelliferyl-alpha-D-mannopyranoside pH 5.0, 37°C, LN-18 cell layer Homo sapiens

Organism

Organism UniProt Comment Textmining
Canavalia sp.
-
-
-
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HCE cell
-
Homo sapiens
-
LN-18 cell
-
Homo sapiens
-
LNZ-308 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-methylumbelliferyl-alpha-D-mannopyranoside + H2O
-
Homo sapiens 4-methylumbelliferone + D-mannose
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000135
-
(2R,3R,4S)-2-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidine-3,4-diol 37°C, pH 5.5 Canavalia sp.
0.000155
-
(1S,2R,8R,8aR)-octahydroindolizine-1,2,8-triol 37°C, pH 5.5 Canavalia sp.
0.000206
-
(3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)-1-methylpyrrolidin-2-one 37°C, pH 5.5 Canavalia sp.
0.004
-
(3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidin-2-one 37°C, pH 5.5 Canavalia sp.

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00001
-
pH 5.0, 37°C, HCEC cell layer Homo sapiens (1S,2R,8R,8aR)-octahydroindolizine-1,2,8-triol
0.00002
-
pH 5.0, 37°C, LNZ-308 cell layer Homo sapiens (1S,2R,8R,8aR)-octahydroindolizine-1,2,8-triol
0.00005
-
pH 5.0, 37°C, LN-18 cell layer Homo sapiens (1S,2R,8R,8aR)-octahydroindolizine-1,2,8-triol
0.0005
-
pH 5.0, 37°C, HCEC cell layer Homo sapiens (3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)-1-methylpyrrolidin-2-one
0.0005
-
pH 5.0, 37°C, LNZ-308 cell layer Homo sapiens (3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)-1-methylpyrrolidin-2-one
0.002
-
pH 5.0, 37°C, LN-18 cell layer Homo sapiens (3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)-1-methylpyrrolidin-2-one
0.025
-
pH 5.0, 37°C, HCEC cell layer Homo sapiens (2R,3R,4S)-2-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidine-3,4-diol
0.05
-
pH 5.0, 37°C, LN-18 cell layer Homo sapiens (2R,3R,4S)-2-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidine-3,4-diol
0.05
-
pH 5.0, 37°C, LNZ-308 cell layer Homo sapiens (2R,3R,4S)-2-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidine-3,4-diol
0.05
-
pH 5.0, 37°C, LNZ-308 cell layer Homo sapiens (3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidin-2-one
0.075
-
pH 5.0, 37°C, HCEC cell layer Homo sapiens (3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidin-2-one
0.35
-
pH 5.0, 37°C, LN-18 cell layer Homo sapiens (3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidin-2-one