Cloned (Comment) | Organism |
---|---|
through pET21b expression vector | Thermotoga maritima |
through pET21b expression vector | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
F59A | slow tight-binding inhibition, affinity for compound 1 comparable to the wild-type level | Thermotoga maritima |
L191A | slow tight-binding inhibition, kinetics like wild type, affinity for compound 1 comparable to the wild-type level | Thermotoga maritima |
M225A | slow tight-binding inhibition, kinetics like wild type, affinity for compound 1 comparable to the wild-type level | Thermotoga maritima |
W58A | instabile | Thermotoga maritima |
Y267A | affinity for compound 1 comparable to the wild-type level | Thermotoga maritima |
Y64A | affinity for compound 1 comparable to the wild-type level | Thermotoga maritima |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(2R,3R,4R,5R,6S)-2-(aminomethyl)-6-methylpiperidine-3,4,5-triol | - |
Homo sapiens | |
(2S,3R,4R,5R)-5-(3-aminopropoxy)-2-methylpiperidine-3,4-diol | - |
Homo sapiens | |
(2S,3R,4R,5R,6S)-2-(hydroxymethyl)-6-methylpiperidine-3,4,5-triol | - |
Homo sapiens | |
(2S,3R,4S,5R)-1-(3-aminopropyl)-2-methylpiperidine-3,4,5-triol | - |
Homo sapiens | |
(2S,3R,4S,5R)-2-benzylpiperidine-3,4,5-triol | - |
Homo sapiens | |
(2S,3R,4S,5R)-2-isopropylpiperidine-3,4,5-triol | - |
Homo sapiens | |
2-cyclopentyl-2-phenyl-N-(((2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methylpiperidin-2-yl)methyl)acetamide | - |
Homo sapiens | |
2-phenyl-N-(((2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methylpiperidin-2-yl)methyl)quinoline-4-carboxamide | - |
Homo sapiens | |
3-(1H-indol-3-yl)-N-(((2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methylpiperidin-2-yl)methyl)propanamide | - |
Homo sapiens | |
5-fluoro-N-(((2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methylpiperidin-2-yl)methyl)-1H-indole-2-carboxamide | - |
Homo sapiens | |
fuconojirimycin | majority of C1-substituted fuconojirimycins act as reversible inhibitors of the human fucosidase | Homo sapiens | |
fuconojirimycin | majority of C1-substituted fuconojirimycins are slow tight-binding inhibitors of the Thermotoga enzyme, Tyr64 and Tyr267 are critically involved in closely interacting with the aglycon of inhibitors | Thermotoga maritima |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P04066 | - |
- |
Thermotoga maritima | - |
- |
- |
Purification (Comment) | Organism |
---|---|
by ion-exchange chromatography, more than 95% homogeneity | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
4-methylumbelliferyl alpha-L-fucopyranoside + H2O | - |
Thermotoga maritima | 4-methylumbelliferone + alpha-L-fucose | - |
? | |
4-methylumbelliferyl alpha-L-fucopyranoside + H2O | - |
Homo sapiens | 4-methylumbelliferone + alpha-L-fucose | - |
? | |
p-nitrophenyl-alpha-L-fucopyranoside + H2O | - |
Thermotoga maritima | p-nitrophenol + alpha-L-fucose | - |
? | |
p-nitrophenyl-alpha-L-fucopyranoside + H2O | - |
Homo sapiens | p-nitrophenol + alpha-L-fucose | - |
? |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0000056 | - |
3-(1H-indol-3-yl)-N-(((2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methylpiperidin-2-yl)methyl)propanamide | - |
Homo sapiens | |
0.0000097 | - |
5-fluoro-N-(((2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methylpiperidin-2-yl)methyl)-1H-indole-2-carboxamide | - |
Homo sapiens | |
0.0000117 | - |
2-phenyl-N-(((2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methylpiperidin-2-yl)methyl)quinoline-4-carboxamide | - |
Homo sapiens | |
0.0000152 | - |
(2R,3R,4R,5R,6S)-2-(aminomethyl)-6-methylpiperidine-3,4,5-triol | - |
Homo sapiens | |
0.000018 | - |
2-cyclopentyl-2-phenyl-N-(((2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methylpiperidin-2-yl)methyl)acetamide | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000052 | - |
- |
Homo sapiens | (2S,3R,4R,5R,6S)-2-(hydroxymethyl)-6-methylpiperidine-3,4,5-triol | |
0.000064 | - |
- |
Homo sapiens | (2R,3R,4R,5R,6S)-2-(aminomethyl)-6-methylpiperidine-3,4,5-triol | |
0.00007 | - |
- |
Homo sapiens | (2S,3R,4S,5R)-1-(3-aminopropyl)-2-methylpiperidine-3,4,5-triol | |
0.000267 | - |
- |
Homo sapiens | (2S,3R,4R,5R)-5-(3-aminopropoxy)-2-methylpiperidine-3,4-diol | |
0.006 | - |
- |
Homo sapiens | (2S,3R,4S,5R)-2-isopropylpiperidine-3,4,5-triol | |
0.007 | - |
- |
Homo sapiens | (2S,3R,4S,5R)-2-benzylpiperidine-3,4,5-triol |