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Literature summary for 3.6.1.54 extracted from

  • Bohl, T.; Ieong, P.; Lee, J.; Lee, T.; Kankanala, J.; Shi, K.; Demir, A.; Kurahashi, K.; Amaro, R.; Wang, Z.; Aihara, H.
    The substrate-binding cap of the UDP-diacylglucosamine pyrophosphatase LpxH is highly flexible, enabling facile substrate binding and product release (2018), J. Biol. Chem., 293, 7969-7981 .
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
DMSO 112% activity at 10% (v/v) DMSO Escherichia coli

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21(DE3) cells Escherichia coli

Crystallization (Commentary)

Crystallization (Comment) Organism
mutant enzyme F141H/L142S/L146S/F147H/E14A/E15A/K161T/E162A, hanging drop vapor diffusion method, using 0.1 M Tris-HCl, pH 8.2, 70-80 mM magnesium formate and 1-5% (v/v) 2-propanol Escherichia coli

Protein Variants

Protein Variants Comment Organism
F141H/L142S/L146S/F147H/E14A/E15A/K161T/E162A solubilized enzyme version with 488% activity compared to the wild type enzyme, including four solubilizing mutations (F141H, L142S, L146S, and F147H) and four surface entropy reduction mutations (E14A, E15A, K161T, and E162A) to improve protein expression and crystallization Escherichia coli
I47C/R149C the mutant shows 141% activity compared to the wild type enzyme Escherichia coli
I47G/R149G the mutant shows 11.3% activity compared to the wild type enzyme Escherichia coli
W136H the mutant shows 600% activity compared to the wild type enzyme Escherichia coli

Inhibitors

Inhibitors Comment Organism Structure
1-(5-((4-(3-(trifluoromethyl) phenyl)piperazin-1-yl) sulfonyl)indolin-1-yl)ethan-1-one 47.2% residual activity at 0.002 mM, 23.5% residual activity at 0.006 mM, 14.1% residual activity at 0.01 mM, 11.7% residual activity at 0.05 mM Escherichia coli

Metals/Ions

Metals/Ions Comment Organism Structure
Mn2+ contains two Mn2+ ions in the active site Escherichia coli

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
UDP-2-N,3-O-bis[(3R)-3-hydroxytetradecanoyl]-alpha-D-glucosamine + H2O Escherichia coli
-
2-N,3-O-bis[(3R)-3-hydroxytetradecanoyl]-alpha-D-glucosaminyl 1-phosphate + UMP
-
?

Organism

Organism UniProt Comment Textmining
Escherichia coli P43341
-
-

Purification (Commentary)

Purification (Comment) Organism
Ni-NTA column chromatography and Superdex 200 gel filtration Escherichia coli

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
UDP-2-N,3-O-bis[(3R)-3-hydroxytetradecanoyl]-alpha-D-glucosamine + H2O
-
Escherichia coli 2-N,3-O-bis[(3R)-3-hydroxytetradecanoyl]-alpha-D-glucosaminyl 1-phosphate + UMP
-
?

Synonyms

Synonyms Comment Organism
LpxH
-
Escherichia coli
UDP-diacylglucosamine pyrophosphatase
-
Escherichia coli

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0012
-
at pH 8.0 and 30°C Escherichia coli 1-(5-((4-(3-(trifluoromethyl) phenyl)piperazin-1-yl) sulfonyl)indolin-1-yl)ethan-1-one