Literature summary for 5.1.3.2 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.

Search for more literature for 5.1.3.2

Application

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

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/ Products (Substrates)

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

Organism	UniProt	Comment	Textmining
Homo sapiens	-	CHO-K1	-
Homo sapiens CHO-K1	-	CHO-K1	-
Trypanosoma brucei	-	-	-

Substrates and Products (Substrate)

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

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

IC50 Value

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

Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.

Release 2023.1 (January 2023)