Application | Comment | Organism |
---|---|---|
drug development | LpxA is a potential target for antibacterial drug discovery | Escherichia coli |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
DL-3-hydroxymyristic acid | competitive versus TAMRA peptide | Escherichia coli | |
HM-UNAG peptide | - |
Escherichia coli | |
HMA peptide | - |
Escherichia coli | |
additional information | development of a fluorescence polarization assay, detecting displacement of a fluorescently labeled peptide inhibitor, based on inhibitor peptide 920 C-terminal 12 residues WMLDPIAGKWSR, by active site ligands, for high-throughput screening of LpxA competitve inhibitors, overview. Abilities of several ligands to compete with TAMRA peptide for binding to Escherichia coli LpxA. Acyl carrier protein does not significantly affect the inhibitory potencies | Escherichia coli | |
peptide 920 | i.e. pentadecapeptide 920, with C-terminus WMLDPIAGKWSR, competitive versus peptide inhibitors derived from its own C-terminal sequence | Escherichia coli | |
TAMRA peptide | ability of the TAMRA-peptide to inhibit the catalytic activity | Escherichia coli | |
UDP-3-O-(R-3-hydroxymyristoyl)-N-acetylglucosamine | competitive versus TAMRA peptide | Escherichia coli | |
UDP-N-acetylglucosamine | competitive versus TAMRA peptide | Escherichia coli | |
UNAG peptide | - |
Escherichia coli |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
an (R)-3-hydroxytetradecanoyl-[acyl-carrier protein] + UDP-N-acetyl-alpha-D-glucosamine | Escherichia coli | - |
an [acyl-carrier protein] + UDP-3-O-(3-hydroxytetradecanoyl)-N-acetyl-alpha-D-glucosamine | - |
r |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Escherichia coli | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
an (R)-3-hydroxytetradecanoyl-[acyl-carrier protein] + UDP-N-acetyl-alpha-D-glucosamine | - |
Escherichia coli | an [acyl-carrier protein] + UDP-3-O-(3-hydroxytetradecanoyl)-N-acetyl-alpha-D-glucosamine | - |
r | |
additional information | development of a fluorescence polarization assay, detecting displacement of a fluorescently labeled peptide inhibitor based on the previously reported inhibitor peptide 920 by active site ligands, for high-throughput screening of LpxA competitve inhibitors, overview | Escherichia coli | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
LpxA | - |
Escherichia coli |
UDP-N-acetylglucosamine acyltransferase | - |
Escherichia coli |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
22 | - |
assay at room temperature | Escherichia coli |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7 | - |
assay at, binding measurements are performed at pH 8.0 | Escherichia coli |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00006 | - |
forward reaction, pH 7.0, 22°C, versus TAMRA peptide | Escherichia coli | peptide 920 | |
0.00014 | - |
forward reaction, pH 7.0, 22°C, versus TAMRA peptide, in absence of holo-ACP | Escherichia coli | HM-UNAG peptide | |
0.00015 | - |
forward reaction, pH 7.0, 22°C | Escherichia coli | TAMRA peptide | |
0.0002 | - |
pH 7.0, 22°C | Escherichia coli | UDP-3-O-(R-3-hydroxymyristoyl)-N-acetylglucosamine | |
0.000238 | - |
forward reaction, pH 7.0, 22°C, versus TAMRA peptide, in presence of holo-ACP | Escherichia coli | HM-UNAG peptide | |
0.00051 | - |
forward reaction, pH 7.0, 22°C, versus TAMRA peptide, in presence of holo-ACP | Escherichia coli | peptide 920 | |
0.0006 | - |
forward reaction, pH 7.0, 22°C, versus 0.001 mM UNAG peptide | Escherichia coli | peptide 920 | |
0.00073 | - |
forward reaction, pH 7.0, 22°C, versus TAMRA peptide, in absence of holo-ACP | Escherichia coli | peptide 920 | |
0.000923 | - |
forward reaction, pH 7.0, 22°C, versus 5 mM UNAG peptide | Escherichia coli | peptide 920 | |
0.047 | - |
forward reaction, pH 7.0, 22°C, versus TAMRA peptide, in absence of holo-ACP | Escherichia coli | HMA peptide | |
0.05 | - |
pH 7.0, 22°C | Escherichia coli | DL-3-hydroxymyristic acid | |
0.063 | - |
forward reaction, pH 7.0, 22°C, versus TAMRA peptide, in presence of holo-ACP | Escherichia coli | HMA peptide | |
5.8 | - |
forward reaction, pH 7.0, 22°C, versus TAMRA peptide, in absence of holo-ACP | Escherichia coli | UNAG peptide | |
6 | - |
pH 7.0, 22°C | Escherichia coli | UDP-N-acetylglucosamine | |
6.6 | - |
forward reaction, pH 7.0, 22°C, versus TAMRA peptide, in presence of holo-ACP | Escherichia coli | UNAG peptide |
General Information | Comment | Organism |
---|---|---|
metabolism | LpxA is the first enzyme in the biosynthetic pathway for the Lipid A component of the outer membrane lipopolysaccharide | Escherichia coli |
physiological function | LpxA catalyzes the condensation of UDP N-acetylglucosamine with R-3-hydroxymyristic acid from R-3-hydroxymyristoyl-acyl carrier protein in the biosynthesis of lipopolysaccharide | Escherichia coli |