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Literature summary extracted from

  • Heath, R.J.; Li, J.; Roland, G.E.; Rock, C.O.
    Inhibition of the Staphylococcus aureus NADPH-dependent enoyl-acyl carrier protein reductase by triclosan and hexachlorophene (2000), J. Biol. Chem., 275, 4654-4659.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.3.1.10 fabI of strain RN4220 found by homology and cloned into pET15b for his-tagged overexpression Staphylococcus aureus
1.3.1.104 expression in Escherichia coli Staphylococcus aureus

Protein Variants

EC Number Protein Variants Comment Organism
1.3.1.10 G93V leads to triclosan resistance Escherichia coli
1.3.1.104 G23S mutation increases the resistance of Staphylococcus aureus to triclosan by an order of magnitude Staphylococcus aureus

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.3.1.10 Hexachlorophene half-maximal inhibition at 0.004 mM Staphylococcus aureus
1.3.1.10 triclosan half-maximal inhibition at 0.003 mM; slow-binding inhibitor forms a stable, ternary complex with enzyme and NADP+ Staphylococcus aureus
1.3.1.104 Hexachlorophene
-
 Staphylococcus aureus
1.3.1.104 triclosan the introduction of a plasmid expressing the enzyme gene leads to triclosan resistance Staphylococcus aureus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.3.1.10 additional information
-
 NADPH value above 2 mM Escherichia coli
1.3.1.10 additional information
-
 NADPH half-maximal rate at 0.065 mM NADPH Staphylococcus aureus
1.3.1.10 additional information
-
 NADPH cooperative binding with Hill coefficient 2.2 Staphylococcus aureus
1.3.1.10 8
-
 Crotonyl-N-acetyl-cysteamine Vmax 0.0003 nmol/min/mg Staphylococcus aureus
1.3.1.104 8
-
 crotonyl-N-acetylcysteamine pH 7.5, 25°C Staphylococcus aureus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.3.1.10 additional information Escherichia coli part of fatty acid synthesis reducing double bonds of a great varity of acyl thioesters ?
-
 ?
1.3.1.10 additional information Staphylococcus aureus part of fatty acid synthesis reducing double bonds of a great varity of acyl thioesters ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.3.1.10 Escherichia coli
-
-
-
1.3.1.10 Staphylococcus aureus Q9RMI3 as there is no information concerning the stereochemistry of hydrogen transfer from NADPH to substrate an appointment to EC 1.3.1.10 or EC 1.3.1.39 is impossible
-
1.3.1.104 Staphylococcus aureus Q9RMI3
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.3.1.10 Ni2+ affinity chromatography on his-tagged protein Staphylococcus aureus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.3.1.10 crotonyl-N-acetyl-cysteamine + NADPH
-
 Staphylococcus aureus butyryl-N-acetyl-cysteamine + NADP+
-
 ?
1.3.1.10 additional information part of fatty acid synthesis reducing double bonds of a great varity of acyl thioesters Escherichia coli ?
-
 ?
1.3.1.10 additional information part of fatty acid synthesis reducing double bonds of a great varity of acyl thioesters Staphylococcus aureus ?
-
 ?
1.3.1.10 octenoyl-N-acetyl-cysteamine + NADPH
-
 Staphylococcus aureus octanoyl-N-acetyl-cysteamine + NADP+
-
 ?
1.3.1.104 crotonyl-N-acetylcysteamine + NADPH + H+
-
 Staphylococcus aureus butyryl-N-acetylcysteamine + NADP+
-
 ?
1.3.1.104 trans-2-octenoyl-N-acetylcysteamine + NADPH + H+
-
 Staphylococcus aureus octanoyl-N-acetylcysteamine + NADP+
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.3.1.104 FabI
-
 Staphylococcus aureus

Cofactor

EC Number Cofactor Comment Organism Structure
1.3.1.10 additional information enzyme is highly specific for NADH, even if isolated at pH 6.5 Escherichia coli
1.3.1.104 NADPH exhibits specific and positive cooperative binding of NADPH. The cofactor concentration that yields 50% of the maximal rate is 65 microM Staphylococcus aureus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.3.1.104 0.003
-
 pH 7.5, 25°C Staphylococcus aureus triclosan

General Information

EC Number General Information Comment Organism
1.3.1.104 physiological function expression complements the Escherichia coli fabI temperature-sensitive mutant Staphylococcus aureus