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Literature summary extracted from

  • Yao, J.; Maxwell, J.B.; Rock, C.O.
    Resistance to AFN-1252 arises from missense mutations in Staphylococcus aureus enoyl-acyl carrier protein reductase (FabI) (2013), J. Biol. Chem., 288, 36261-36271 .
    View publication on PubMedView publication on EuropePMC

Protein Variants

EC Number Protein Variants Comment Organism
1.3.1.104 M99T mutant is resistant to antibiotic AFN-1252 but susceptible to triclosan. Strains expressing M99T exhibit normal growth, and the biochemical properties of the purified protein are indistinguishable from those of FabI Staphylococcus aureus
1.3.1.104 Y147H mutant is resistant to antibiotic AFN-1252 and to triclosan, about 5% of wild-type catalytic activity. A strain expressing Y147H has a pronounced growth defect that is rescued by exogenous fatty acid supplementation Staphylococcus aureus

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.3.1.104 AFN-1252 antibiotic AFN-1252, i.e. (2E)-N-methyl-N-[(3-methyl-1-benzofuran-2-yl)methyl]-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)prop-2-enamide, only binds to the NADPH form of FabI Staphylococcus aureus

Organism

EC Number Organism UniProt Comment Textmining
1.3.1.104 Staphylococcus aureus Q9RMI3
-
-
1.3.1.104 Staphylococcus aureus RN4220 Q9RMI3
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.3.1.104 crotonyl-[acyl-carrier-protein] + NADPH + H+
-
 Staphylococcus aureus butyryl-[acyl-carrier-protein] + NADP+
-
 ?
1.3.1.104 crotonyl-[acyl-carrier-protein] + NADPH + H+
-
 Staphylococcus aureus RN4220 butyryl-[acyl-carrier-protein] + NADP+
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.3.1.104 FabI
-
 Staphylococcus aureus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.3.1.104 0.004
-
 AFN-1252 wild-type, pH 7.8, 30°C Staphylococcus aureus
1.3.1.104 0.069
-
 AFN-1252 mutant M99T, pH 7.8, 30°C Staphylococcus aureus