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Literature summary 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

EC Number Application Comment Organism
2.3.1.41 pharmacology synthase III is a target for drug development against multi-drug resistant strains Staphylococcus aureus
2.3.1.180 medicine the enzyme is a target of antibacterial treatment of the pathogen Staphylococcus aureus Staphylococcus aureus
2.3.1.180 pharmacology the enzyme is a target for development of inhibitors for treatment of the multi-drug resistant pathogen Staphylococcus aureus Staphylococcus aureus

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.3.1.41 synthase III, overexpression of His-tagged FabH in Escherichia coli BL21 (DE3) Staphylococcus aureus
2.3.1.180 gene fabH, overexpression of N-terminal His-tagged enzyme in Escherichia coli strain BL21(DE3) Staphylococcus aureus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.41 4-phenyl-5-phenylimino-[1,2,4]dithiazolidin-3-one i.e. HR19; strong, synthase III Staphylococcus aureus
2.3.1.41 5-chloro-4-phenyl-[1,2]-dithiol-3-one complete inhibition at 0.01 nM, synthase III; i.e. HR12 Staphylococcus aureus
2.3.1.41 cerulenin weak, synthase III Staphylococcus aureus
2.3.1.41 thiolactomycin synthase III; weak Staphylococcus aureus
2.3.1.180 4-phenyl-5-phenylimino-[1,2,4]dithiazolidin-3-one CAS-No. 5338-82-9, IC50 is 0.00078 mM Staphylococcus aureus
2.3.1.180 5-chloro-4-phenyl-[1,2]-dithiol-3-one CAS-No. 2425-05-0, IC50 is 0.0019 mM Staphylococcus aureus
2.3.1.180 cerulenin
-
 Staphylococcus aureus
2.3.1.180 additional information antibacterial potency of inhibitors, overview Staphylococcus aureus
2.3.1.180 thiolactomycin weak inhibition, IC50 is above 0.1 mM Staphylococcus aureus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.3.1.41 0.00032
-
 isobutyryl-CoA synthase III Staphylococcus aureus
2.3.1.41 0.00232
-
 butyryl-CoA synthase III Staphylococcus aureus
2.3.1.41 0.00618
-
 acetyl-CoA synthase III Staphylococcus aureus
2.3.1.180 0.0003
-
 isobutyryl-CoA pH 7.2, 30°C, recombinant enzyme Staphylococcus aureus
2.3.1.180 0.0023
-
 butyryl-CoA pH 7.2, 30°C, recombinant enzyme Staphylococcus aureus
2.3.1.180 0.0062
-
 acetyl-CoA pH 7.2, 30°C, recombinant enzyme Staphylococcus aureus

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.3.1.41 additional information
-
 amino acid sequence alignment Staphylococcus aureus
2.3.1.41 37000
-
 2 * 37000, recombinant synthase III, SDS-PAGE Staphylococcus aureus
2.3.1.41 67600
-
 gel filtration Staphylococcus aureus
2.3.1.180 37000
-
 2 * 37000, recombinant enzyme, SDS-PAGE Staphylococcus aureus
2.3.1.180 66700
-
 recombinant enzyme, gel filtration Staphylococcus aureus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.3.1.41 acyl-[acyl-carrier protein] + malonyl-[acyl-carrier protein] Staphylococcus aureus initiation of fatty acid biosynthesis 3-oxoacyl-[acyl-carrier protein] + CO2 + [acyl-carrier protein]
-
 ir
2.3.1.41 acyl-[acyl-carrier protein] + malonyl-[acyl-carrier protein] Staphylococcus aureus part of fatty acid synthase II 3-oxoacyl-[acyl-carrier protein] + CO2 + [acyl-carrier protein]
-
 ir
2.3.1.180 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

EC Number Organism UniProt Comment Textmining
2.3.1.41 Staphylococcus aureus P99159 synthase III, gene fabH
-
2.3.1.41 Staphylococcus aureus P99159 strain ATCC 35556
-
2.3.1.180 Staphylococcus aureus
-
 single-copy gene fabH
-

Posttranslational Modification

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

Purification (Commentary)

EC Number Purification (Comment) Organism
2.3.1.41 recombinant His-tagged synthase III from E. coli Staphylococcus aureus
2.3.1.180 recombinant His-tagged enzyme from Escherichia coli strain BL21(DE3) by nickel affinity chromatography and gel filtration Staphylococcus aureus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.41 acetyl-CoA + malonyl-[acyl-carrier protein]
-
 Staphylococcus aureus ?
-
 ?
2.3.1.41 acetyl-[acyl-carrier protein] + malonyl-[acyl-carrier protein] synthase III Staphylococcus aureus acetoacyl-[acyl-carrier protein] + CO2 + [acyl-carrier protein]
-
 ir
2.3.1.41 acyl-[acyl-carrier protein] + malonyl-[acyl-carrier protein] initiation of fatty acid biosynthesis Staphylococcus aureus 3-oxoacyl-[acyl-carrier protein] + CO2 + [acyl-carrier protein]
-
 ir
2.3.1.41 acyl-[acyl-carrier protein] + malonyl-[acyl-carrier protein] part of fatty acid synthase II Staphylococcus aureus 3-oxoacyl-[acyl-carrier protein] + CO2 + [acyl-carrier protein]
-
 ir
2.3.1.41 butyryl-CoA + malonyl-[acyl-carrier protein]
-
 Staphylococcus aureus ?
-
 ?
2.3.1.41 butyryl-[acyl-carrier protein] + malonyl-[acyl-carrier protein] synthase III Staphylococcus aureus beta-ketohexanoyl-[acyl-carrier protein] + CO2 + [acyl-carrier protein]
-
 ?
2.3.1.41 isobutyryl-CoA + malonyl-[acyl-carrier protein] synthase III Staphylococcus aureus ?
-
 ?
2.3.1.41 saturated acyl-[acyl-carrier protein] + malonyl-[acyl-carrier protein]
-
 Staphylococcus aureus 3-oxoacyl-[acyl-carrier protein] + CO2 + [acyl-carrier protein]
-
 ir
2.3.1.180 acetyl-CoA + malonyl-[acyl-carrier protein]
-
 Staphylococcus aureus acetoacetyl-[acyl-carrier protein] + CoA + CO2
-
 ?
2.3.1.180 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
-
 ?
2.3.1.180 butyryl-CoA + malonyl-[acyl-carrier protein]
-
 Staphylococcus aureus 3-oxo-hexanoyl-[acyl-carrier protein] + CoA + CO2
-
 ?
2.3.1.180 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

EC Number Subunits Comment Organism
2.3.1.41 dimer 2 * 37000, recombinant synthase III, SDS-PAGE Staphylococcus aureus
2.3.1.180 dimer 2 * 37000, recombinant enzyme, SDS-PAGE Staphylococcus aureus

Synonyms

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

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.3.1.180 30
-
 assay at Staphylococcus aureus

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.3.1.180 0.27
-
 acetyl-CoA pH 7.2, 30°C, recombinant enzyme Staphylococcus aureus
2.3.1.180 0.72
-
 butyryl-CoA pH 7.2, 30°C, recombinant enzyme Staphylococcus aureus
2.3.1.180 1.63
-
 isobutyryl-CoA pH 7.2, 30°C, recombinant enzyme Staphylococcus aureus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.3.1.41 7.2
-
 synthase III Staphylococcus aureus
2.3.1.180 7.2
-
 assay at Staphylococcus aureus

pH Range

EC Number pH Minimum pH Maximum Comment Organism
2.3.1.41 5.8 8 synthase III Staphylococcus aureus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.180 0.00078
-
 CAS-No. 5338-82-9, IC50 is 0.00078 mM Staphylococcus aureus 4-phenyl-5-phenylimino-[1,2,4]dithiazolidin-3-one
2.3.1.180 0.0019
-
 CAS-No. 2425-05-0, IC50 is 0.0019 mM Staphylococcus aureus 5-chloro-4-phenyl-[1,2]-dithiol-3-one
2.3.1.180 0.1
-
 weak inhibition, IC50 is above 0.1 mM Staphylococcus aureus thiolactomycin