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Literature summary for 1.3.1.104 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

Protein Variants Comment Organism
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
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

Inhibitors Comment Organism Structure
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

Organism UniProt Comment Textmining
Staphylococcus aureus Q9RMI3
-
-
Staphylococcus aureus RN4220 Q9RMI3
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
FabI
-
Staphylococcus aureus

Ki Value [mM]

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