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Literature summary extracted from

  • Maccari, R.; Ciurleo, R.; Giglio, M.; Cappiello, M.; Moschini, R.; Corso, A.D.; Mura, U.; Ottana, R.
    Identification of new non-carboxylic acid containing inhibitors of aldose reductase (2010), Bioorg. Med. Chem., 18, 4049-4055.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.21 (Z)-5-(naphthalen-1-ylmethylidene)-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione 52% inhibition at 0.025 mM Bos taurus
1.1.1.21 (Z)-5-(naphthalen-2-ylmethylidene)-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione 59% inhibition at 0.025 mM Bos taurus
1.1.1.21 (Z)-5-[(3-hydroxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
 Bos taurus
1.1.1.21 (Z)-5-[(3-methoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
 Bos taurus
1.1.1.21 (Z)-5-[(3-phenoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione 64% inhibition at 0.025 mM Bos taurus
1.1.1.21 (Z)-5-[(4-hydroxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
 Bos taurus
1.1.1.21 (Z)-5-[(4-methoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
 Bos taurus
1.1.1.21 (Z)-5-[(4-phenoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
 Bos taurus
1.1.1.21 (Z)-5-[(4-phenylphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione 45% inhibition at 0.025 mM Bos taurus
1.1.1.21 epalrestat
-
 Bos taurus
1.1.1.21 fidarestat
-
 Bos taurus
1.1.1.21 lidorestat
-
 Bos taurus
1.1.1.21 additional information synthesis and evaluation of 2,4-thiazolidinedione inhibitors, structure-activity relationships, overview. No inhibition by (Z)-5-[(4-benzyloxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione Bos taurus
1.1.1.21 sorbinil
-
 Bos taurus
1.1.1.21 Tolrestat
-
 Bos taurus
1.1.1.21 zopolrestat
-
 Bos taurus

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.21 Bos taurus
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.1.1.21 native enzyme from lens by anion exchange and Matrex Orange A affinity chromatography Bos taurus

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.21 lens
-
 Bos taurus
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
1.1.1.21 0.93
-
 purified enzyme, pH 6.8, 37°C Bos taurus

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
1.1.1.21 aldose reductase
-
 Bos taurus
1.1.1.21 ALR2
-
 Bos taurus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.1.1.21 37
-
 assay at Bos taurus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.1.1.21 6.8
-
 assay at Bos taurus

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.21 NADPH
-
 Bos taurus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.21 0.002
-
 pH 6.8, 37°C Bos taurus sorbinil
1.1.1.21 0.003
-
 pH 6.8, 37°C Bos taurus (Z)-5-[(4-hydroxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
1.1.1.21 0.0083
-
 pH 6.8, 37°C Bos taurus (Z)-5-[(4-phenoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
1.1.1.21 0.0123
-
 pH 6.8, 37°C Bos taurus (Z)-5-[(3-hydroxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
1.1.1.21 0.0174
-
 pH 6.8, 37°C Bos taurus (Z)-5-[(4-methoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
1.1.1.21 0.0233
-
 pH 6.8, 37°C Bos taurus (Z)-5-[(3-methoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione