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Literature summary for 2.5.1.7 extracted from

  • Jin, B.S.; Han, S.G.; Lee, W.K.; Ryoo, S.W.; Lee, S.J.; Suh, S.W.; Yu, Y.G.
    Inhibitory mechanism of novel inhibitors of UDP-N-acetylglucosamine enolpyruvyl transferase from Haemophilus influenzae (2009), J. Microbiol. Biotechnol., 19, 1582-1589.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
coding region of Haemophilus influenzae MurA is cloned into the NdeI and XhoI sites of pET21a to generate an expression vector for MurA, the expression vector is transformed into Escherichia coli Rosetta2 (DE3), and the recombinant MurA is expressed Haemophilus influenzae

Inhibitors

Inhibitors Comment Organism Structure
ebselen inhibitor covalently modifies the cysteine residue near the active site-loop of MurA, modification changes the open conformation of MurA to a more closed configuration, when compound is incubated for 30 min with dithiothreitol, its inhibitory activity against Haemophilus influenzae MurA is completely eliminated Haemophilus influenzae
fosfomycin
-
Haemophilus influenzae
thimerosal inhibitor covalently modifies the cysteine residue near the active site-loop of MurA, modification changes the open conformation of MurA to a more closed configuration, when compound is incubated for 30 min with dithiothreitol, its inhibitory activity against Haemophilus influenzae MurA is completely eliminated Haemophilus influenzae
thiram inhibitor covalently modifies the cysteine residue near the active site-loop of MurA, modification changes the open conformation of MurA to a more closed configuration, when compound is incubated for 30 min with dithiothreitol, its inhibitory activity against Haemophilus influenzae MurA is completely eliminated Haemophilus influenzae

Organism

Organism UniProt Comment Textmining
Haemophilus influenzae P45025
-
-

Synonyms

Synonyms Comment Organism
MurA
-
Haemophilus influenzae
UDP-N-acetylglucosamine enolpyruvyl transferase
-
Haemophilus influenzae

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Haemophilus influenzae

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0001
-
50 mM Tris-HCl, pH 7.8, compound displays an anti-MurA activity that is above 90% at a concentration below 0.002 mM Haemophilus influenzae ebselen
0.0004
-
50 mM Tris-HCl, pH 7.8, compound displays an anti-MurA activity that is above 90% at a concentration below 0.002 mM Haemophilus influenzae thimerosal
0.0007
-
50 mM Tris-HCl, pH 7.8, compound displays an anti-MurA activity that is above 90% at a concentration below 0.002 mM Haemophilus influenzae thiram
0.04
-
50 mM Tris-HCl, pH 7.8, compound displays an anti-MurA activity that is above 90% at a concentration below 0.002 mM Haemophilus influenzae fosfomycin

General Information

General Information Comment Organism
physiological function enzyme catalyzes the first step of bacterial cell wall synthesis Haemophilus influenzae