Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 1.1.1.21 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

Inhibitors Comment Organism Structure
(Z)-5-(naphthalen-1-ylmethylidene)-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione 52% inhibition at 0.025 mM Bos taurus
(Z)-5-(naphthalen-2-ylmethylidene)-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione 59% inhibition at 0.025 mM Bos taurus
(Z)-5-[(3-hydroxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
Bos taurus
(Z)-5-[(3-methoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
Bos taurus
(Z)-5-[(3-phenoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione 64% inhibition at 0.025 mM Bos taurus
(Z)-5-[(4-hydroxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
Bos taurus
(Z)-5-[(4-methoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
Bos taurus
(Z)-5-[(4-phenoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
Bos taurus
(Z)-5-[(4-phenylphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione 45% inhibition at 0.025 mM Bos taurus
epalrestat
-
Bos taurus
fidarestat
-
Bos taurus
lidorestat
-
Bos taurus
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
sorbinil
-
Bos taurus
Tolrestat
-
Bos taurus
zopolrestat
-
Bos taurus

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-

Purification (Commentary)

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

Source Tissue

Source Tissue Comment Organism Textmining
lens
-
Bos taurus
-

Specific Activity [micromol/min/mg]

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

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
aldose reductase
-
Bos taurus
ALR2
-
Bos taurus

Temperature Optimum [°C]

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

pH Optimum

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

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Bos taurus

IC50 Value

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