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Literature summary extracted from

  • Mochalkin, I.; Lightle, S.; Narasimhan, L.; Bornemeier, D.; Melnick, M.; Vanderroest, S.; McDowell, L.
    Structure of a small-molecule inhibitor complexed with GlmU from Haemophilus influenzae reveals an allosteric binding site (2008), Protein Sci., 17, 577-582.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.3.1.157 expressed in Escherichia coli as a GST-fusion protein Mycobacterium tuberculosis
2.7.7.23 expressed in Escherichia coli Haemophilus influenzae

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.3.1.157 crystallized using the hanging drop vapour-diffusion method. Native diffraction data are collected from crystals belonging to space group R32 and processed to a resolution of 2.2 A Mycobacterium tuberculosis
2.7.7.23 a 1.9 A resolution crystal structure of a synthetic small-molecule inhibitor (4-chloro-N-(3-methoxypropyl)-N-[1-(2-phenylethyl)piperidin-3-yl]benzamide) of GlmU is presented. The determined crystal structure indicate that the inhibitor occupies an allosteric site adjacent to the GlcNAc-1-P substrate-binding region, thus, preventing structural rearrangements that are required for the enzymatic reaction Haemophilus influenzae

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.7.23 4-chloro-N-(3-methoxypropyl)-N-[1-(2-phenylethyl)piperidin-3-yl]benzamide a 1.9 A resolution crystal structure of this synthetic small-molecule inhibitor of GlmU is presented. The determined crystal structure indicates that the inhibitor occupies an allosteric site adjacent to the GlcNAc-1-P substrate-binding region, thus, preventing structural rearrangements that are required for the enzymatic reaction Haemophilus influenzae
2.7.7.23 4-chloro-N-[1-[2-(2-fluorophenyl)ethyl]piperidin-3-yl]-N-(3-methoxypropyl)benzamide
-
 Haemophilus influenzae
2.7.7.23 4-chloro-N-[1-[2-(3-fluorophenyl)ethyl]piperidin-3-yl]-N-(3-methoxypropyl)benzamide
-
 Haemophilus influenzae
2.7.7.23 4-chloro-N-[1-[2-(4-fluorophenyl)ethyl]piperidin-3-yl]-N-(3-methoxypropyl)benzamide
-
 Haemophilus influenzae
2.7.7.23 4-fluoro-N-(3-methoxypropyl)-N-[1-(2-phenylethyl)piperidin-3-yl]benzamide
-
 Haemophilus influenzae

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.7.23 Mg2+
-
 Haemophilus influenzae

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.157 Mycobacterium tuberculosis
-
-
-
2.7.7.23 Haemophilus influenzae P43889
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.3.1.157 using a GSTrap glutathione Sepharose column. The GST tag is removed by proteolytic cleavage using recombinant tobacco etch virus protease Mycobacterium tuberculosis

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.7.23 UTP + N-acetylglucosamine 1-phosphate
-
 Haemophilus influenzae diphosphate + UDP-N-acetyl-D-glucosamine
-
 ?

Subunits

EC Number Subunits Comment Organism
2.3.1.157 homotrimer crystal structure Mycobacterium tuberculosis

Synonyms

EC Number Synonyms Comment Organism
2.3.1.157 MtbGlmU
-
 Mycobacterium tuberculosis
2.3.1.157 Rv1018c
-
 Mycobacterium tuberculosis
2.7.7.23 hiGlmU
-
 Haemophilus influenzae

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.7.7.23 7.5
-
 assay at Haemophilus influenzae

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.7.23 0.018
-
-
 Haemophilus influenzae 4-chloro-N-(3-methoxypropyl)-N-[1-(2-phenylethyl)piperidin-3-yl]benzamide
2.7.7.23 0.02
-
-
 Haemophilus influenzae 4-fluoro-N-(3-methoxypropyl)-N-[1-(2-phenylethyl)piperidin-3-yl]benzamide
2.7.7.23 0.089
-
-
 Haemophilus influenzae 4-chloro-N-[1-[2-(4-fluorophenyl)ethyl]piperidin-3-yl]-N-(3-methoxypropyl)benzamide
2.7.7.23 0.1
-
 value above Haemophilus influenzae 4-chloro-N-[1-[2-(2-fluorophenyl)ethyl]piperidin-3-yl]-N-(3-methoxypropyl)benzamide
2.7.7.23 0.1
-
 value above Haemophilus influenzae 4-chloro-N-[1-[2-(3-fluorophenyl)ethyl]piperidin-3-yl]-N-(3-methoxypropyl)benzamide