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Literature summary for 2.3.1.129 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

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

Inhibitors

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/ Products (Substrates)

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

Organism UniProt Comment Textmining
Escherichia coli
-
-
-

Substrates and Products (Substrate)

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

Synonyms Comment Organism
LpxA
-
Escherichia coli
UDP-N-acetylglucosamine acyltransferase
-
Escherichia coli

Temperature Optimum [°C]

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

pH Optimum

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 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

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