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

BRENDA support

Literature summary extracted from

  • Van Zandt, M.C.; Doan, B.; Sawicki, D.R.; Sredy, J.; Podjarny, A.D.
    Discovery of [3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acids as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications (2009), Bioorg. Med. Chem. Lett., 19, 2006-2008.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.1.21 expression of ALR2 in Escherichia coli Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.1.1.21 purified recombinant ALR2, with the oxidized form of beta-NADPH, pH 5.0, 4°C, X-ray diffraction structure determination and analysis at 1.8 A resolution Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.21 lidorestat
-
 Homo sapiens
1.1.1.21 additional information development of series of highly potent and selective [3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid aldose reductase inhibitors. The compounds inhibit aldose reductase, but are inactive against aldehyde reductase Homo sapiens
1.1.1.21 [3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
-
 Homo sapiens
1.1.1.21 [6-ethyl-3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
-
 Homo sapiens
1.1.1.21 [6-methyl-3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.21 D-glucose + NADPH + H+ Homo sapiens aldose reductase, ALR2 sorbitol + NADP+
-
 ?
1.1.1.21 sorbitol + NAD+ Homo sapiens aldehyde reductase, ALR1 D-fructose + NADH + H+
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.21 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.21 D-glucose + NADPH + H+ aldose reductase, ALR2 Homo sapiens sorbitol + NADP+
-
 ?
1.1.1.21 sorbitol + NAD+ aldehyde reductase, ALR1 Homo sapiens D-fructose + NADH + H+
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.21 aldehyde reductase
-
 Homo sapiens
1.1.1.21 aldose reductase
-
 Homo sapiens
1.1.1.21 ALR1
-
 Homo sapiens
1.1.1.21 ALR2
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.21 NAD+
-
 Homo sapiens
1.1.1.21 NADP+
-
 Homo sapiens
1.1.1.21 NADPH
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.21 0.000005
-
 ALR2, pH not specified in the publication, temperature not specified in the publication Homo sapiens lidorestat
1.1.1.21 0.000007
-
 ALR2, pH not specified in the publication, temperature not specified in the publication Homo sapiens [3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
1.1.1.21 0.000008
-
 ALR2, pH not specified in the publication, temperature not specified in the publication Homo sapiens [6-methyl-3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
1.1.1.21 0.000012
-
 ALR2, pH not specified in the publication, temperature not specified in the publication Homo sapiens [6-ethyl-3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
1.1.1.21 0.027
-
 ALR1, pH not specified in the publication, temperature not specified in the publication Homo sapiens lidorestat
1.1.1.21 0.1
-
 above, ALR1, pH not specified in the publication, temperature not specified in the publication Homo sapiens [3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
1.1.1.21 0.1
-
 above, ALR1, pH not specified in the publication, temperature not specified in the publication Homo sapiens [6-methyl-3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
1.1.1.21 0.1012
-
 above, ALR1, pH not specified in the publication, temperature not specified in the publication Homo sapiens [6-ethyl-3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid

General Information

EC Number General Information Comment Organism
1.1.1.21 metabolism aldose reductase, ALR2, and aldehyde reductase, ALR1, catalyse two following steps in the polyol pathway, overview Homo sapiens