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Literature summary for 1.3.1.9 extracted from

  • Takahata, S.; Iida, M.; Yoshida, T.; Kumura, K.; Kitagawa, H.; Hoshiko, S.
    Discovery of 4-pyridone derivatives as specific inhibitors of enoyl-acyl carrier protein reductase (FabI) with antibacterial activity against Staphylococcus aureus (2007), J. Antibiot., 60, 123-128.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli Top10 cells Staphylococcus aureus
expressed in Escherichia coli Top10 cells Escherichia coli

Protein Variants

Protein Variants Comment Organism
A95V aureus triclosan-resistant mutant Staphylococcus aureus
A95V aureus triclosan-resistant mutant Escherichia coli
G93V coli triclosan-resistant mutant Escherichia coli

Inhibitors

Inhibitors Comment Organism Structure
1-(3-chlorobenzyl)-3-(2,6-dichlorobenzyl)-2-methylpyridin-4(1H)-one
-
Escherichia coli
1-(3-chlorobenzyl)-3-(2,6-dichlorobenzyl)-2-methylpyridin-4(1H)-one
-
Staphylococcus aureus
3-(2,6-dichlorobenzyl)-2-methyl-1-(2-methyl-2-[[3-(trifluoromethyl)benzyl]sulfanyl]propyl)pyridin-4(1H)-one
-
Escherichia coli
3-(2,6-dichlorobenzyl)-2-methyl-1-(thiophen-2-ylmethyl)pyridin-4(1H)-one
-
Escherichia coli
3-(2,6-dichlorobenzyl)-2-methyl-1-(thiophen-2-ylmethyl)pyridin-4(1H)-one
-
Staphylococcus aureus
triclosan
-
Escherichia coli
triclosan
-
Staphylococcus aureus

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-
Staphylococcus aureus
-
strain ATCC 29213
-

Purification (Commentary)

Purification (Comment) Organism
Ni-NTA agarose column chromatography Staphylococcus aureus
Ni-NTA agarose column chromatography Escherichia coli

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
crotonyl-CoA + NADH + H+
-
Staphylococcus aureus butyryl-CoA + NAD+
-
?
crotonyl-CoA + NADH + H+
-
Escherichia coli butyryl-CoA + NAD+
-
?

Synonyms

Synonyms Comment Organism
enoyl-acyl carrier protein reductase
-
Staphylococcus aureus
enoyl-acyl carrier protein reductase
-
Escherichia coli
FabI
-
Staphylococcus aureus
FabI
-
Escherichia coli

Cofactor

Cofactor Comment Organism Structure
NADH
-
Staphylococcus aureus
NADH
-
Escherichia coli

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00034
-
in 0.1 M sodium N-(2-acetamido)-iminodiacetic acid (pH 6.5) Staphylococcus aureus 1-(3-chlorobenzyl)-3-(2,6-dichlorobenzyl)-2-methylpyridin-4(1H)-one
0.00034
-
wild type enzyme, in 0.1 M sodium N-(2-acetamido)-iminodiacetic acid (pH 6.5) Escherichia coli 1-(3-chlorobenzyl)-3-(2,6-dichlorobenzyl)-2-methylpyridin-4(1H)-one
0.00035
-
in 0.1 M sodium N-(2-acetamido)-iminodiacetic acid (pH 6.5) Staphylococcus aureus 3-(2,6-dichlorobenzyl)-2-methyl-1-(thiophen-2-ylmethyl)pyridin-4(1H)-one
0.0004
-
wild type enzyme, in 0.1 M sodium N-(2-acetamido)-iminodiacetic acid (pH 6.5) Escherichia coli 3-(2,6-dichlorobenzyl)-2-methyl-1-(thiophen-2-ylmethyl)pyridin-4(1H)-one
0.00051
-
wild type enzyme, in 0.1 M sodium N-(2-acetamido)-iminodiacetic acid (pH 6.5) Escherichia coli triclosan
0.0018
-
wild type enzyme, in 0.1 M sodium N-(2-acetamido)-iminodiacetic acid (pH 6.5) Escherichia coli 3-(2,6-dichlorobenzyl)-2-methyl-1-(2-methyl-2-[[3-(trifluoromethyl)benzyl]sulfanyl]propyl)pyridin-4(1H)-one
0.0033
-
mutant enzyme G93V, in 0.1 M sodium N-(2-acetamido)-iminodiacetic acid (pH 6.5) Escherichia coli 1-(3-chlorobenzyl)-3-(2,6-dichlorobenzyl)-2-methylpyridin-4(1H)-one
0.0038
-
in 0.1 M sodium N-(2-acetamido)-iminodiacetic acid (pH 6.5) Staphylococcus aureus triclosan
0.0099
-
mutant enzyme G93V, in 0.1 M sodium N-(2-acetamido)-iminodiacetic acid (pH 6.5) Escherichia coli triclosan
0.038
-
mutant enzyme G93V, in 0.1 M sodium N-(2-acetamido)-iminodiacetic acid (pH 6.5) Escherichia coli 3-(2,6-dichlorobenzyl)-2-methyl-1-(thiophen-2-ylmethyl)pyridin-4(1H)-one