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Literature summary for 1.1.1.21 extracted from

  • Manzanaro, S.; Salva, J.; de la Fuente, J.A.
    Phenolic marine natural products as aldose reductase inhibitors (2006), J. Nat. Prod., 69, 1485-1487.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(4-hydroxyphenyl)(6-hydroxypyrazin-2-yl)methanone isolated from red ascidian Botryllus leachi, pyrazine derivative, IC50: 0.0414 mM Homo sapiens
(4-hydroxyphenyl)[4-(4-hydroxyphenyl)-1H-imidazol-2-yl]methanone isolated from red ascidian Botryllus leachi, imidazole derivative, IC50: 0.0214 mM Homo sapiens
(5Z)-3-chloro-4-(3,5-dibromo-4-hydroxyphenyl)-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]furan-2(5H)-one isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.019 mM Homo sapiens
(5Z)-3-chloro-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]-4-(4-hydroxyphenyl)furan-2(5H)-one isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.0008 mM Homo sapiens
(5Z)-4-(3,5-dibromo-4-hydroxyphenyl)-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]furan-2(5H)-one isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.020 mM Homo sapiens
(5Z)-4-(3-bromo-4-hydroxyphenyl)-3-chloro-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]furan-2(5H)-one isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.013 mM Homo sapiens
(5Z)-4-(3-bromo-4-hydroxyphenyl)-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]furan-2(5H)-one isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.048 mM Homo sapiens
(5Z)-4-(3-bromo-4-hydroxyphenyl)-5-[(3-bromo-4-hydroxyphenyl)methylidene]-3-chlorofuran-2(5H)-one isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.017 mM Homo sapiens
(5Z)-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]-4-(4-hydroxyphenyl)furan-2(5H)-one isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.057 mM Homo sapiens
(5Z)-5-[(3-bromo-4-hydroxyphenyl)methylidene]-3-chloro-4-(4-hydroxyphenyl)furan-2(5H)-one isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.046 mM Homo sapiens
epalrestat orally active inhibitor Homo sapiens
lukianol B IC50: 0.0006 mM Homo sapiens
sorbinil orally active inhibitor, IC50: 0.0036 mM Homo sapiens
Tolrestat orally active inhibitor Homo sapiens
Zenarestat orally active inhibitor Homo sapiens
[6-hydroxy-3-(4-hydroxyphenoxy)pyrazin-2-yl](4-hydroxyphenyl)methanone isolated from red ascidian Botryllus leachi, pyrazine derivative, IC50: 0.0194 mM Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
aldose + NADPH + H+ Homo sapiens
-
alditol + NADP+
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
aldose + NADPH + H+
-
Homo sapiens alditol + NADP+
-
?

Synonyms

Synonyms Comment Organism
aldose reductase
-
Homo sapiens
ALR2
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6.2
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0006
-
IC50: 0.0006 mM Homo sapiens lukianol B
0.0008
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.0008 mM Homo sapiens (5Z)-3-chloro-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]-4-(4-hydroxyphenyl)furan-2(5H)-one
0.0036
-
orally active inhibitor, IC50: 0.0036 mM Homo sapiens sorbinil
0.013
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.013 mM Homo sapiens (5Z)-4-(3-bromo-4-hydroxyphenyl)-3-chloro-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]furan-2(5H)-one
0.017
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.017 mM Homo sapiens (5Z)-4-(3-bromo-4-hydroxyphenyl)-5-[(3-bromo-4-hydroxyphenyl)methylidene]-3-chlorofuran-2(5H)-one
0.019
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.019 mM Homo sapiens (5Z)-3-chloro-4-(3,5-dibromo-4-hydroxyphenyl)-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]furan-2(5H)-one
0.0194
-
isolated from red ascidian Botryllus leachi, pyrazine derivative, IC50: 0.0194 mM Homo sapiens [6-hydroxy-3-(4-hydroxyphenoxy)pyrazin-2-yl](4-hydroxyphenyl)methanone
0.02
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.020 mM Homo sapiens (5Z)-4-(3,5-dibromo-4-hydroxyphenyl)-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]furan-2(5H)-one
0.0214
-
isolated from red ascidian Botryllus leachi, imidazole derivative, IC50: 0.0214 mM Homo sapiens (4-hydroxyphenyl)[4-(4-hydroxyphenyl)-1H-imidazol-2-yl]methanone
0.0414
-
isolated from red ascidian Botryllus leachi, pyrazine derivative, IC50: 0.0414 mM Homo sapiens (4-hydroxyphenyl)(6-hydroxypyrazin-2-yl)methanone
0.046
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.046 mM Homo sapiens (5Z)-5-[(3-bromo-4-hydroxyphenyl)methylidene]-3-chloro-4-(4-hydroxyphenyl)furan-2(5H)-one
0.048
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.048 mM Homo sapiens (5Z)-4-(3-bromo-4-hydroxyphenyl)-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]furan-2(5H)-one
0.057
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.057 mM Homo sapiens (5Z)-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]-4-(4-hydroxyphenyl)furan-2(5H)-one