Application | Comment | Organism |
---|---|---|
medicine | Trypanosoma brucei GalE is a validated drug target for African sleeping sickness. The Trypanosoma brucei enzyme can be selectively inhibited by small molecules that are not substrate analogues in vitro, although the mechanism of cytotoxicity of these inhibitors is unconfirmed. Of the compounds screened, ethacrynic acid displays the best therapeutic index, but is clinically used as a loop diuretic and was found to form multiple covalent adducts with TbGalE in vitro, limiting its potential as a lead compound. | Trypanosoma brucei |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
bisprasin | - |
Trypanosoma brucei | |
diamino(dimethylamino)methyl (E)-{(8alpha,13E,14alpha)-14-[2-(furan-3-yl)ethyl]-8-methylpodocarpan-13-ylidene}methyl sulfate | - |
Homo sapiens | |
diamino(dimethylamino)methyl (E)-{(8alpha,13E,14alpha)-14-[2-(furan-3-yl)ethyl]-8-methylpodocarpan-13-ylidene}methyl sulfate | - |
Trypanosoma brucei | |
diethylstilbestrol | - |
Homo sapiens | |
diethylstilbestrol | - |
Trypanosoma brucei | |
ebselen | - |
Homo sapiens | |
ebselen | - |
Trypanosoma brucei | |
Ethacrynic acid | - |
Homo sapiens | |
Ethacrynic acid | - |
Trypanosoma brucei | |
haloprogin | - |
Homo sapiens | |
haloprogin | - |
Trypanosoma brucei | |
psammaplin A | - |
Homo sapiens | |
psammaplin A | - |
Trypanosoma brucei |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
UDP-alpha-D-glucose | Homo sapiens | The enzyme UDP-glucose 4'-epimerase (GalE) interconverts UDP-glucose (UDP-Glc) and UDP-galactose (UDP-Gal). | UDP-alpha-D-galactose | - |
r | |
UDP-alpha-D-glucose | Trypanosoma brucei | The enzyme UDP-glucose 4'-epimerase (GalE) interconverts UDP-glucose (UDP-Glc) and UDP-galactose (UDP-Gal). | UDP-alpha-D-galactose | - |
r | |
UDP-alpha-D-glucose | Homo sapiens CHO-K1 | The enzyme UDP-glucose 4'-epimerase (GalE) interconverts UDP-glucose (UDP-Glc) and UDP-galactose (UDP-Gal). | UDP-alpha-D-galactose | - |
r |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
CHO-K1 | - |
Homo sapiens CHO-K1 | - |
CHO-K1 | - |
Trypanosoma brucei | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
UDP-alpha-D-glucose | The enzyme UDP-glucose 4'-epimerase (GalE) interconverts UDP-glucose (UDP-Glc) and UDP-galactose (UDP-Gal). | Homo sapiens | UDP-alpha-D-galactose | - |
r | |
UDP-alpha-D-glucose | The enzyme UDP-glucose 4'-epimerase (GalE) interconverts UDP-glucose (UDP-Glc) and UDP-galactose (UDP-Gal). | Trypanosoma brucei | UDP-alpha-D-galactose | - |
r | |
UDP-alpha-D-glucose | The enzyme UDP-glucose 4'-epimerase (GalE) interconverts UDP-glucose (UDP-Glc) and UDP-galactose (UDP-Gal). | Homo sapiens CHO-K1 | UDP-alpha-D-galactose | - |
r |
Synonyms | Comment | Organism |
---|---|---|
TbGalE | - |
Trypanosoma brucei |
UDP-Glc 4-epimerase | - |
Homo sapiens |
UDP-Glc 4-epimerase | - |
Trypanosoma brucei |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.014 | - |
- |
Homo sapiens | ebselen | |
0.5 | - |
- |
Homo sapiens | haloprogin | |
0.62 | - |
- |
Trypanosoma brucei | ebselen | |
3.1 | - |
- |
Trypanosoma brucei | Ethacrynic acid | |
3.6 | - |
- |
Homo sapiens | psammaplin A | |
5.6 | - |
- |
Trypanosoma brucei | diamino(dimethylamino)methyl (E)-{(8alpha,13E,14alpha)-14-[2-(furan-3-yl)ethyl]-8-methylpodocarpan-13-ylidene}methyl sulfate | |
12 | - |
- |
Homo sapiens | diamino(dimethylamino)methyl (E)-{(8alpha,13E,14alpha)-14-[2-(furan-3-yl)ethyl]-8-methylpodocarpan-13-ylidene}methyl sulfate | |
13 | - |
- |
Trypanosoma brucei | haloprogin | |
14 | - |
- |
Homo sapiens | Ethacrynic acid | |
14 | - |
- |
Trypanosoma brucei | bisprasin | |
15 | - |
- |
Trypanosoma brucei | psammaplin A | |
17 | - |
- |
Trypanosoma brucei | diethylstilbestrol | |
75 | - |
- |
Homo sapiens | diethylstilbestrol |