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Literature summary extracted from

  • Li, L.; Chang, K.C.; Zhou, Y.; Shieh, B.; Ponder, J.; Abraham, A.D.; Ali, H.; Snow, A.; Petrash, J.M.; LaBarbera, D.V.
    Design of an amide N-glycoside derivative of beta-glucogallin: a stable, potent, and specific inhibitor of aldose reductase (2014), J. Med. Chem., 57, 71-77.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.21 1-O-Galloyl-beta-D-glucose i.e. beta-glucogallin or BGG, a major component of the Emblica officinalis medicinal plant, and a stable, potent, and specific inhibitor of aldose reductase, noncompetitive inhibition through binding the active site of AKR1B1, occupying both the anionic and the specificity pockets Homo sapiens
1.1.1.21 1-O-Galloyl-beta-D-glucose i.e. beta-glucogallin or BGG, a major component of the Emblica officinalis medicinal plant, and a stable, potent, and specific inhibitor of aldose reductase, noncompetitive inhibition through binding the active site of AKR1B1, occupying both the anionic and the specificity pockets Mus musculus
1.1.1.21 additional information no inhibition by the triazole 1-(beta-D-glucopyranosyl)-4-(3,4,5-trihydroxyphenyl)-1,2,3-triazole, the amide N-phenylacetyl beta-D-glucopyranosylamine, and the glycosides of beta-glucogallin, 2-(3,4,5-trihydroxyphenyl)ethyl beta-D-glucopyranoside, [1-(3,4,5-trihydroxybenzyl)-1,2,3-triazole-4-yl]methyl beta-D-glucopyranoside, and 3-(3,4,5-trihydroxyphenyl)propyl beta-D-glucopyranoside, synthesis and evaluation, overview Homo sapiens
1.1.1.21 additional information no inhibition by the triazole 1-(beta-D-glucopyranosyl)-4-(3,4,5-trihydroxyphenyl)-1,2,3-triazole, the amide N-phenylacetyl beta-D-glucopyranosylamine, and the glycosides of beta-glucogallin, 2-(3,4,5-trihydroxyphenyl)ethyl beta-D-glucopyranoside, [1-(3,4,5-trihydroxybenzyl)-1,2,3-triazole-4-yl]methyl beta-D-glucopyranoside, and 3-(3,4,5-trihydroxyphenyl)propyl beta-D-glucopyranoside, synthesis and evaluation, overview Mus musculus
1.1.1.21 N-galloyl beta-D-glucopyranosylamine
-
 Homo sapiens
1.1.1.21 N-galloyl beta-D-glucopyranosylamine
-
 Mus musculus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.21 glyceraldehyde + NADPH + H+ Homo sapiens
-
 glycerol + NADP+
-
 ?
1.1.1.21 glyceraldehyde + NADPH + H+ Mus musculus
-
 glycerol + NADP+
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.21 Homo sapiens P15121
-
-
1.1.1.21 Mus musculus P45376
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.21 lens
-
 Mus musculus
-
1.1.1.21 macrophage
-
 Mus musculus
-
1.1.1.21 RAW-264.7 cell
-
 Mus musculus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.21 glyceraldehyde + NADPH + H+
-
 Homo sapiens glycerol + NADP+
-
 ?
1.1.1.21 glyceraldehyde + NADPH + H+
-
 Mus musculus glycerol + NADP+
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.21 AKR1B1
-
 Homo sapiens
1.1.1.21 AKR1B1
-
 Mus musculus
1.1.1.21 aldose reductase
-
 Homo sapiens
1.1.1.21 aldose reductase
-
 Mus musculus

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.21 NADPH dependent on Homo sapiens
1.1.1.21 NADPH dependent on Mus musculus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.21 0.008
-
 pH and temperature not specified in the publication Homo sapiens 1-O-Galloyl-beta-D-glucose
1.1.1.21 0.009
-
 pH and temperature not specified in the publication Homo sapiens N-galloyl beta-D-glucopyranosylamine

General Information

EC Number General Information Comment Organism
1.1.1.21 evolution aldose reductase (AKR1B1) is a member of the aldo-keto reductase superfamily Mus musculus
1.1.1.21 evolution human aldose reductase (AKR1B1) is a member of the aldo-keto reductase superfamily, which consists of 15 families, 3 of which are mammalian containing the thirteen human aldo-keto reductase enzymes currently identified Homo sapiens
1.1.1.21 metabolism AKR1B1 functions in the polyol pathway as an NADPH-dependent enzyme, catalyzing the reduction of glucose to sorbitol, which is then converted to fructose by sorbitol dehydrogenase Homo sapiens
1.1.1.21 metabolism AKR1B1 functions in the polyol pathway as an NADPH-dependent enzyme, catalyzing the reduction of glucose to sorbitol, which is then converted to fructose by sorbitol dehydrogenase Mus musculus