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