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

BRENDA support

Literature summary for 1.1.1.21 extracted from

  • Rakowitz, D.; Maccari, R.; Ottana, R.; Vigorita, M.G.
    In vitro aldose reductase inhibitory activity of 5-benzyl-2,4-thiazolidinediones (2006), Bioorg. Med. Chem., 14, 567-574.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(5-biphenyl-4-ylmethyl-2,4-dioxothiazolidin-3-yl)acetic acid IC50: 0.0017 mM Bos taurus
(5-biphenyl-4-ylmethyl-2,4-dioxothiazolidin-3-yl)acetic acid methyl ester 15% inhibition of ALR2 at 0.05 mM Bos taurus
5-(3-methoxybenzyl)-2,4-thiazolidinedione 16% inhibition of ALR2 at 0.05 mM Bos taurus
5-(3-phenoxybenzyl)-2,4-thiazolidinedione IC50: 0.0789 mM Bos taurus
5-(4-benzyloxybenzyl)-2,4-thiazolidinedione IC50: 0.0314 mM Bos taurus
5-(4-methoxybenzyl)-2,4-thiazolidinedione 21% inhibition of ALR2 at 0.05 mM Bos taurus
5-(4-phenoxybenzyl)-2,4-thiazolidinedione IC50: 0.0404 mM Bos taurus
5-biphenyl-4-ylmethyl-2,4-thiazolidinedione IC50: 0.0658 mM Bos taurus
epalrestat
-
Bos taurus
additional information poor inhibition by [2,4-dioxo-5-(4-phenoxybenzyl)thiazolidin-3-yl]acetic acid methyl ester Bos taurus
pioglitazone
-
Bos taurus
ponalrestat IC50: 80 nM Bos taurus
rosiglitazone
-
Bos taurus
sorbinil IC50: 0.0034 mM Bos taurus
[2,4-dioxo-5-(3-phenoxybenzyl)thiazolidin-3-yl]acetic acid IC50: 0.0010 mM Bos taurus
[2,4-dioxo-5-(3-phenoxybenzyl)thiazolidin-3-yl]acetic acid methyl ester 26% inhibition of ALR2 at 0.05 mM Bos taurus
[2,4-dioxo-5-(4-phenoxybenzyl)thiazolidin-3-yl]acetic acid IC50: 0.0028 mM Bos taurus
[5-(3-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid IC50: 0.0030 mM Bos taurus
[5-(3-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester IC50: 0.0211 mM Bos taurus
[5-(4-benzyloxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester 24% inhibition of ALR2 at 0.05 mM Bos taurus
[5-(4-hydroxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid IC50: 0.0021 mM Bos taurus
[5-(4-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid IC50: 0.0011 mM Bos taurus
[5-(4-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester 24% inhibition of ALR2 at 0.05 mM Bos taurus

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
lens
-
Bos taurus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
glyceraldehyde + NADPH + H+
-
Bos taurus 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
7
-
assay at Bos taurus

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Bos taurus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00008
-
IC50: 80 nM Bos taurus ponalrestat
0.001
-
IC50: 0.0010 mM Bos taurus [2,4-dioxo-5-(3-phenoxybenzyl)thiazolidin-3-yl]acetic acid
0.0011
-
IC50: 0.0011 mM Bos taurus [5-(4-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid
0.0017
-
IC50: 0.0017 mM Bos taurus (5-biphenyl-4-ylmethyl-2,4-dioxothiazolidin-3-yl)acetic acid
0.0021
-
IC50: 0.0021 mM Bos taurus [5-(4-hydroxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid
0.0028
-
IC50: 0.0028 mM Bos taurus [2,4-dioxo-5-(4-phenoxybenzyl)thiazolidin-3-yl]acetic acid
0.003
-
IC50: 0.0030 mM Bos taurus [5-(3-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid
0.0034
-
IC50: 0.0034 mM Bos taurus sorbinil
0.0211
-
IC50: 0.0211 mM Bos taurus [5-(3-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester
0.0314
-
IC50: 0.0314 mM Bos taurus 5-(4-benzyloxybenzyl)-2,4-thiazolidinedione
0.0404
-
IC50: 0.0404 mM Bos taurus 5-(4-phenoxybenzyl)-2,4-thiazolidinedione
0.0658
-
IC50: 0.0658 mM Bos taurus 5-biphenyl-4-ylmethyl-2,4-thiazolidinedione
0.0789
-
IC50: 0.0789 mM Bos taurus 5-(3-phenoxybenzyl)-2,4-thiazolidinedione