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Literature summary for 2.3.1.180 extracted from

  • He, X.; Reynolds, K.A.
    Purification, characterization, and identification of novel inhibitors of the beta-ketoacyl-acyl carrier protein synthase III (FabH) from Staphylococcus aureus (2002), Antimicrob. Agents Chemother., 46, 1310-1318.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine the enzyme is a target of antibacterial treatment of the pathogen Staphylococcus aureus Staphylococcus aureus
pharmacology the enzyme is a target for development of inhibitors for treatment of the multi-drug resistant pathogen Staphylococcus aureus Staphylococcus aureus

Cloned(Commentary)

Cloned (Comment) Organism
gene fabH, overexpression of N-terminal His-tagged enzyme in Escherichia coli strain BL21(DE3) Staphylococcus aureus

Inhibitors

Inhibitors Comment Organism Structure
4-phenyl-5-phenylimino-[1,2,4]dithiazolidin-3-one CAS-No. 5338-82-9, IC50 is 0.00078 mM Staphylococcus aureus
5-chloro-4-phenyl-[1,2]-dithiol-3-one CAS-No. 2425-05-0, IC50 is 0.0019 mM Staphylococcus aureus
cerulenin
-
Staphylococcus aureus
additional information antibacterial potency of inhibitors, overview Staphylococcus aureus
thiolactomycin weak inhibition, IC50 is above 0.1 mM Staphylococcus aureus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0003
-
isobutyryl-CoA pH 7.2, 30°C, recombinant enzyme Staphylococcus aureus
0.0023
-
butyryl-CoA pH 7.2, 30°C, recombinant enzyme Staphylococcus aureus
0.0062
-
acetyl-CoA pH 7.2, 30°C, recombinant enzyme Staphylococcus aureus

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
37000
-
2 * 37000, recombinant enzyme, SDS-PAGE Staphylococcus aureus
66700
-
recombinant enzyme, gel filtration Staphylococcus aureus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
acetyl-CoA + malonyl-[acyl-carrier protein] Staphylococcus aureus the enzyme is involved in initiation of fatty acid elogantion by the fatty acid synthase II catalyzing the decarboxylative condensation between malonyl-ACP and acetyl-CoA, the enzyme is essential for viability, overview acetoacetyl-[acyl-carrier protein] + CoA + CO2
-
?

Organism

Organism UniProt Comment Textmining
Staphylococcus aureus
-
single-copy gene fabH
-

Posttranslational Modification

Posttranslational Modification Comment Organism
no modification strain MRSA, N315, and strain VRSA, Mu 50 Staphylococcus aureus

Purification (Commentary)

Purification (Comment) Organism
recombinant His-tagged enzyme from Escherichia coli strain BL21(DE3) by nickel affinity chromatography and gel filtration Staphylococcus aureus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-CoA + malonyl-[acyl-carrier protein]
-
Staphylococcus aureus acetoacetyl-[acyl-carrier protein] + CoA + CO2
-
?
acetyl-CoA + malonyl-[acyl-carrier protein] the enzyme is involved in initiation of fatty acid elogantion by the fatty acid synthase II catalyzing the decarboxylative condensation between malonyl-ACP and acetyl-CoA, the enzyme is essential for viability, overview Staphylococcus aureus acetoacetyl-[acyl-carrier protein] + CoA + CO2
-
?
butyryl-CoA + malonyl-[acyl-carrier protein]
-
Staphylococcus aureus 3-oxo-hexanoyl-[acyl-carrier protein] + CoA + CO2
-
?
isobutyryl-CoA + malonyl-[acyl-carrier protein] isobutyryl-CoA is the preferred CoA primer substrate Staphylococcus aureus 3-oxo-4-methyl-pentanoyl-[acyl-carrier protein] + CoA + CO2
-
?

Subunits

Subunits Comment Organism
dimer 2 * 37000, recombinant enzyme, SDS-PAGE Staphylococcus aureus

Synonyms

Synonyms Comment Organism
ACP synthase III
-
Staphylococcus aureus
beta-ketoacyl-acyl carrier protein synthase III
-
Staphylococcus aureus
FabH
-
Staphylococcus aureus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
assay at Staphylococcus aureus

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.27
-
acetyl-CoA pH 7.2, 30°C, recombinant enzyme Staphylococcus aureus
0.72
-
butyryl-CoA pH 7.2, 30°C, recombinant enzyme Staphylococcus aureus
1.63
-
isobutyryl-CoA pH 7.2, 30°C, recombinant enzyme Staphylococcus aureus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.2
-
assay at Staphylococcus aureus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00078
-
CAS-No. 5338-82-9, IC50 is 0.00078 mM Staphylococcus aureus 4-phenyl-5-phenylimino-[1,2,4]dithiazolidin-3-one
0.0019
-
CAS-No. 2425-05-0, IC50 is 0.0019 mM Staphylococcus aureus 5-chloro-4-phenyl-[1,2]-dithiol-3-one
0.1
-
weak inhibition, IC50 is above 0.1 mM Staphylococcus aureus thiolactomycin