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Literature summary extracted from

  • Stefek, M.; Snirc, V.; Djoubissie, P.O.; Majekova, M.; Demopoulos, V.; Rackova, L.; Bezakova, Z.; Karasu, C.; Carbone, V.; El-Kabbani, O.
    Carboxymethylated pyridoindole antioxidants as aldose reductase inhibitors: Synthesis, activity, partitioning, and molecular modeling (2008), Bioorg. Med. Chem., 16, 4908-4920.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.21 (2-benzyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-yl)-acetic acid uncompetitive with both D,L-glyceraldehyde and NADPH Rattus norvegicus
1.1.1.21 (2-phenethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-yl)-acetic acid uncompetitive with both D,L-glyceraldehyde and NADPH Rattus norvegicus
1.1.1.21 zopolrestat
-
 Rattus norvegicus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.1.1.21 0.054
-
 NADPH isoform ALR2, pH 6.2, 30°C Rattus norvegicus
1.1.1.21 0.585
-
 DL-glyceraldehyde isoform ALR2, pH 6.2, 30°C Rattus norvegicus

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.21 Rattus norvegicus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.21 kidney isoform ALR1 Rattus norvegicus
-
1.1.1.21 lens isoform ALR2 Rattus norvegicus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.21 DL-glyceraldehyde + NADPH
-
 Rattus norvegicus glycerol + NADP+
-
 ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.1.1.21 0.000005
-
 zopolrestat pH 6.2, 30°C, isoform ALR2 Rattus norvegicus
1.1.1.21 0.0167
-
 (2-phenethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-yl)-acetic acid pH 6.2, 30°C, isoform ALR2 Rattus norvegicus
1.1.1.21 0.0182
-
 (2-benzyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-yl)-acetic acid pH 6.2, 30°C, isoform ALR2 Rattus norvegicus
1.1.1.21 0.328
-
 (2-phenethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-yl)-acetic acid pH 7.2, 37°C, isoform ALR1 Rattus norvegicus
1.1.1.21 3.081
-
 (2-benzyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-yl)-acetic acid pH 7.2, 37°C, isoform ALR1 Rattus norvegicus