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Literature summary extracted from

  • Shapiro, A.B.; Ross, P.L.; Gao, N.; Livchak, S.; Kern, G.; Yang, W.; Andrews, B.; Thresher, J.
    A high-throughput-compatible fluorescence anisotropy-based assay for competitive inhibitors of Escherichia coli UDP-N-acetylglucosamine acyltransferase (LpxA) (2013), J. Biomol. Screen., 18, 341-347.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.3.1.129 drug development LpxA is a potential target for antibacterial drug discovery Escherichia coli

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.129 DL-3-hydroxymyristic acid competitive versus TAMRA peptide Escherichia coli
2.3.1.129 HM-UNAG peptide
-
 Escherichia coli
2.3.1.129 HMA peptide
-
 Escherichia coli
2.3.1.129 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
2.3.1.129 peptide 920 i.e. pentadecapeptide 920, with C-terminus WMLDPIAGKWSR, competitive versus peptide inhibitors derived from its own C-terminal sequence Escherichia coli
2.3.1.129 TAMRA peptide ability of the TAMRA-peptide to inhibit the catalytic activity Escherichia coli
2.3.1.129 UDP-3-O-(R-3-hydroxymyristoyl)-N-acetylglucosamine competitive versus TAMRA peptide Escherichia coli
2.3.1.129 UDP-N-acetylglucosamine competitive versus TAMRA peptide Escherichia coli
2.3.1.129 UNAG peptide
-
 Escherichia coli

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.3.1.129 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

EC Number Organism UniProt Comment Textmining
2.3.1.129 Escherichia coli
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.129 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
2.3.1.129 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

EC Number Synonyms Comment Organism
2.3.1.129 LpxA
-
 Escherichia coli
2.3.1.129 UDP-N-acetylglucosamine acyltransferase
-
 Escherichia coli

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.3.1.129 22
-
 assay at room temperature Escherichia coli

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.3.1.129 7
-
 assay at, binding measurements are performed at pH 8.0 Escherichia coli

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.129 0.00006
-
 forward reaction, pH 7.0, 22°C, versus TAMRA peptide Escherichia coli peptide 920
2.3.1.129 0.00014
-
 forward reaction, pH 7.0, 22°C, versus TAMRA peptide, in absence of holo-ACP Escherichia coli HM-UNAG peptide
2.3.1.129 0.00015
-
 forward reaction, pH 7.0, 22°C Escherichia coli TAMRA peptide
2.3.1.129 0.0002
-
 pH 7.0, 22°C Escherichia coli UDP-3-O-(R-3-hydroxymyristoyl)-N-acetylglucosamine
2.3.1.129 0.000238
-
 forward reaction, pH 7.0, 22°C, versus TAMRA peptide, in presence of holo-ACP Escherichia coli HM-UNAG peptide
2.3.1.129 0.00051
-
 forward reaction, pH 7.0, 22°C, versus TAMRA peptide, in presence of holo-ACP Escherichia coli peptide 920
2.3.1.129 0.0006
-
 forward reaction, pH 7.0, 22°C, versus 0.001 mM UNAG peptide Escherichia coli peptide 920
2.3.1.129 0.00073
-
 forward reaction, pH 7.0, 22°C, versus TAMRA peptide, in absence of holo-ACP Escherichia coli peptide 920
2.3.1.129 0.000923
-
 forward reaction, pH 7.0, 22°C, versus 5 mM UNAG peptide Escherichia coli peptide 920
2.3.1.129 0.047
-
 forward reaction, pH 7.0, 22°C, versus TAMRA peptide, in absence of holo-ACP Escherichia coli HMA peptide
2.3.1.129 0.05
-
 pH 7.0, 22°C Escherichia coli DL-3-hydroxymyristic acid
2.3.1.129 0.063
-
 forward reaction, pH 7.0, 22°C, versus TAMRA peptide, in presence of holo-ACP Escherichia coli HMA peptide
2.3.1.129 5.8
-
 forward reaction, pH 7.0, 22°C, versus TAMRA peptide, in absence of holo-ACP Escherichia coli UNAG peptide
2.3.1.129 6
-
 pH 7.0, 22°C Escherichia coli UDP-N-acetylglucosamine
2.3.1.129 6.6
-
 forward reaction, pH 7.0, 22°C, versus TAMRA peptide, in presence of holo-ACP Escherichia coli UNAG peptide

General Information

EC Number General Information Comment Organism
2.3.1.129 metabolism LpxA is the first enzyme in the biosynthetic pathway for the Lipid A component of the outer membrane lipopolysaccharide Escherichia coli
2.3.1.129 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