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Literature summary for 2.3.1.41 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

Application Comment Organism
drug development the enzyme is a target for antibacterial drugs Staphylococcus aureus

Inhibitors

Inhibitors Comment Organism Structure
additional information in vivo inhibition assays, no inhibition by platensimycin Staphylococcus aureus
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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Staphylococcus aureus inhibition of FabH leads to loss of accumulation of acetoacetyl-ACP ?
-
?

Organism

Organism UniProt Comment Textmining
Staphylococcus aureus
-
methicillin-resistant and vancomycin-resistant strains
-

Specific Activity [micromol/min/mg]

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

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
beta-ketoacyl-[acyl carrier protein (ACP)] synthase III
-
Staphylococcus aureus
FabH
-
Staphylococcus aureus

Temperature Optimum [°C]

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

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7
-
assay at Staphylococcus aureus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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