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Literature summary extracted from

  • Urbaniak, M.D.; Tabudravu, J.N.; Msaki, A.; Matera, K.M.; Brenk, R.; Jaspars, M.; Ferguson, M.A.
    Identification of novel inhibitors of UDP-Glc 4-epimerase, a validated drug target for african sleeping sickness (2006), Bioorg. Med. Chem. Lett., 16, 5744-5747.
    View publication on PubMed

Application

EC Number Application Comment Organism
5.1.3.2 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

EC Number Inhibitors Comment Organism Structure
5.1.3.2 bisprasin
-
 Trypanosoma brucei
5.1.3.2 diamino(dimethylamino)methyl (E)-{(8alpha,13E,14alpha)-14-[2-(furan-3-yl)ethyl]-8-methylpodocarpan-13-ylidene}methyl sulfate
-
 Homo sapiens
5.1.3.2 diamino(dimethylamino)methyl (E)-{(8alpha,13E,14alpha)-14-[2-(furan-3-yl)ethyl]-8-methylpodocarpan-13-ylidene}methyl sulfate
-
 Trypanosoma brucei
5.1.3.2 diethylstilbestrol
-
 Homo sapiens
5.1.3.2 diethylstilbestrol
-
 Trypanosoma brucei
5.1.3.2 ebselen
-
 Homo sapiens
5.1.3.2 ebselen
-
 Trypanosoma brucei
5.1.3.2 Ethacrynic acid
-
 Homo sapiens
5.1.3.2 Ethacrynic acid
-
 Trypanosoma brucei
5.1.3.2 haloprogin
-
 Homo sapiens
5.1.3.2 haloprogin
-
 Trypanosoma brucei
5.1.3.2 psammaplin A
-
 Homo sapiens
5.1.3.2 psammaplin A
-
 Trypanosoma brucei

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5.1.3.2 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
5.1.3.2 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
5.1.3.2 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

EC Number Organism UniProt Comment Textmining
5.1.3.2 Homo sapiens
-
 CHO-K1
-
5.1.3.2 Homo sapiens CHO-K1
-
 CHO-K1
-
5.1.3.2 Trypanosoma brucei
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.1.3.2 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
5.1.3.2 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
5.1.3.2 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

EC Number Synonyms Comment Organism
5.1.3.2 TbGalE
-
 Trypanosoma brucei
5.1.3.2 UDP-Glc 4-epimerase
-
 Homo sapiens
5.1.3.2 UDP-Glc 4-epimerase
-
 Trypanosoma brucei

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5.1.3.2 0.014
-
-
 Homo sapiens ebselen
5.1.3.2 0.5
-
-
 Homo sapiens haloprogin
5.1.3.2 0.62
-
-
 Trypanosoma brucei ebselen
5.1.3.2 3.1
-
-
 Trypanosoma brucei Ethacrynic acid
5.1.3.2 3.6
-
-
 Homo sapiens psammaplin A
5.1.3.2 5.6
-
-
 Trypanosoma brucei diamino(dimethylamino)methyl (E)-{(8alpha,13E,14alpha)-14-[2-(furan-3-yl)ethyl]-8-methylpodocarpan-13-ylidene}methyl sulfate
5.1.3.2 12
-
-
 Homo sapiens diamino(dimethylamino)methyl (E)-{(8alpha,13E,14alpha)-14-[2-(furan-3-yl)ethyl]-8-methylpodocarpan-13-ylidene}methyl sulfate
5.1.3.2 13
-
-
 Trypanosoma brucei haloprogin
5.1.3.2 14
-
-
 Homo sapiens Ethacrynic acid
5.1.3.2 14
-
-
 Trypanosoma brucei bisprasin
5.1.3.2 15
-
-
 Trypanosoma brucei psammaplin A
5.1.3.2 17
-
-
 Trypanosoma brucei diethylstilbestrol
5.1.3.2 75
-
-
 Homo sapiens diethylstilbestrol