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Literature summary extracted from

  • Wang, J.; Kodali, S.; Lee, S.H.; Galgoci, A.; Painter, R.; Dorso, K.; Racine, F.; Motyl, M.; Hernandez, L.; Tinney, E.; Colletti, S.L.; Herath, K.; Cummings, R.; Salazar, O.; Gonzalez, I.; Basilio, A.; Vicente, F.; Genilloud, O.; Pelaez, F.; Jayasuriya, H.; Young, K.; Cully, D.F.; Singh, S.B.
    Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties (2007), Proc. Natl. Acad. Sci. USA, 104, 7612-7616.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
2.3.1.41 drug development the enzyme is a target for antibacterial drugs Staphylococcus aureus
2.3.1.179 drug development the enzyme is a target for antibacterial drugs Staphylococcus aureus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.41 additional information in vivo inhibition assays, no inhibition by platensimycin Staphylococcus aureus
2.3.1.41 platencin exhibits a broad-spectrum Gram-positive antibacterial activity through inhibition of fatty acid biosynthesis, targets the two essential proteins, beta-ketoacyl-[acyl carrier protein] synthase II and III, i.e. FabF and FabH, purified FabH IC50: 0.016 mM, overview Staphylococcus aureus
2.3.1.179 additional information in vivo inhibition assays Staphylococcus aureus
2.3.1.179 platencin exhibits a broad-spectrum Gram-positive antibacterial activity through inhibition of fatty acid biosynthesis, targets the two essential proteins, beta-ketoacyl-[acyl carrier protein] synthase II and III, i.e. FabF and FabH, FabF IC50: 113 nM, overview Staphylococcus aureus
2.3.1.179 platensimycin from a strain of Streptomyces platensis MA7339, specifically targets FabF, IC50: 290 nM, exhibits Gram-positive antibacterial activity Staphylococcus aureus
2.3.1.180 platencin
-
 Staphylococcus aureus
2.3.1.180 platensimycin
-
 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 additional information Staphylococcus aureus inhibition of FabH leads to loss of accumulation of acetoacetyl-ACP ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.41 Staphylococcus aureus
-
 methicillin-resistant and vancomycin-resistant strains
-
2.3.1.179 Staphylococcus aureus
-
-
-
2.3.1.179 Staphylococcus aureus
-
 methicillin-resistant and vancomycin-resistant strains
-
2.3.1.180 Staphylococcus aureus
-
-
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.3.1.41 additional information
-
 development of an elongation assay with FabF, EC 2.3.1.179, and FabH Staphylococcus aureus
2.3.1.179 additional information
-
 development of an elongation assay with FabF and FabH, EC 2.3.1.41 Staphylococcus aureus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.41 additional information inhibition of FabH leads to loss of accumulation of acetoacetyl-ACP Staphylococcus aureus ?
-
 ?
2.3.1.41 additional information FabH produces C14 long-chain beta-ketoacyl-ACP Staphylococcus aureus ?
-
 ?
2.3.1.179 additional information FabF produces C14 long-chain beta-ketoacyl-ACP Staphylococcus aureus ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.1.41 beta-ketoacyl-[acyl carrier protein (ACP)] synthase III
-
 Staphylococcus aureus
2.3.1.41 FabH
-
 Staphylococcus aureus
2.3.1.179 beta-ketoacyl-[acyl carrier protein (ACP)] synthase II
-
 Staphylococcus aureus
2.3.1.179 beta-ketoacyl-[acyl-carrier protein (ACP)] synthase II
-
 Staphylococcus aureus
2.3.1.179 FabF
-
 Staphylococcus aureus
2.3.1.180 beta-ketoacyl-[acyl-carrier protein (ACP)] 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
2.3.1.41 30
-
 assay at Staphylococcus aureus
2.3.1.179 30
-
 assay at Staphylococcus aureus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.3.1.41 7
-
 assay at Staphylococcus aureus
2.3.1.179 7
-
 assay at Staphylococcus aureus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.41 0.016
-
 exhibits a broad-spectrum Gram-positive antibacterial activity through inhibition of fatty acid biosynthesis, targets the two essential proteins, beta-ketoacyl-[acyl carrier protein] synthase II and III, i.e. FabF and FabH, purified FabH IC50: 0.016 mM, o Staphylococcus aureus platencin
2.3.1.179 additional information
-
 IC50 for platencin is 0.00195 ng/ml, IC50 for platensimycin is 0.00013 ng/ml Staphylococcus aureus additional information
2.3.1.179 0.000113
-
 exhibits a broad-spectrum Gram-positive antibacterial activity through inhibition of fatty acid biosynthesis, targets the two essential proteins, beta-ketoacyl-[acyl carrier protein] synthase II and III, i.e. FabF and FabH, FabF IC50: 113 nM, overview Staphylococcus aureus platencin
2.3.1.179 0.00029
-
 from a strain of Streptomyces platensis MA7339, specifically targets FabF, IC50: 290 nM, exhibits Gram-positive antibacterial activity Staphylococcus aureus platensimycin
2.3.1.180 additional information
-
 IC50 for platencin is 0.00391 ng/ml Staphylococcus aureus additional information