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Literature summary for 5.4.99.9 extracted from

  • Wangkanont, K.; Winton, V.J.; Forest, K.T.; Kiessling, L.L.
    Conformational control of UDP-galactopyranose mutase inhibition (2017), Biochemistry, 56, 3983-3992 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
recombinant expression of C-terminally His6-tagged or GSG-tagged enzyme Corynebacterium diphtheriae

Crystallization (Commentary)

Crystallization (Comment) Organism
purified recombinant His6-tagged enzyme in complex with citrate and GSG-tagged enzyme in complex with UDP, by hanging drop vapor diffusion method, mixing of 0.002 ml of 10 mg/ml protein in 20 mM Tris, pH 7.0, with 0.002 ml of reservoir solution containing for the citrate-complexed enzyme 100 mM sodium citrate, pH 5.6, 15% isopropanol, and 16-18% PEG 5000 MME, for 3-4 days, and containing for the UDP-complexed enzyme 100 mM Bis-Tris, pH 5.5, 200 mM lithium sulfate, and 21% PEG 3350, for 1-2 weeks, X-ray diffraction structure determination and analysis at 1.95-2.35 A resolution, molecular replacement using KpUGM monomer structure in an open conformation (PDB ID 2BI7) as template for the citrate-complexed enzyme crystals and the structure of Mycobacterium smegmatis UGM (MsUGM) in a closed conformation (PDB ID 5EQD) for the UDP-complexed enzyme crystals, structure comparisons, overview Corynebacterium diphtheriae

Inhibitors

Inhibitors Comment Organism Structure
2-((4-(3,4-dichlorophenyl)thiazol-2-yl)amino)-3-(4-iodophenyl)propanoic acid
-
Corynebacterium diphtheriae
3-(4-bromobenzyl)-6-(4-chlorophenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine-7-carboxylic acid
-
Corynebacterium diphtheriae
6-(4-chlorophenyl)-3-(thiophen-2-yl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine-7-carboxylic acid
-
Corynebacterium diphtheriae
additional information the enzyme can be inhibited by 2-aminothiazoles, e.g. 2-((4-(3,4-dichlorophenyl)thiazol-2-yl)amino)-3-(4-iodophenyl)propanoic acid, or triazolothiadiazines, such as 6-(4-chlorophenyl)-3-(thiophen-2-yl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine-7-carboxylic acid or 3-(4-bromobenzyl)-6-(4-chlorophenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine-7-carboxylic acid Corynebacterium diphtheriae

Metals/Ions

Metals/Ions Comment Organism Structure
citrate the citrate ion is identified on the basis of its shape and bonding partners and is located in the active site cavity adjacent to the FAD cofactor. Citrate is anionic like the UDP-alpha-D-galactopyranose substrate. The citrate ion forms salt bridges with UGM residues R288 and H290 and numerous ordered water molecules, thereby participating in a hydrogen-bonding network with the active site residues Corynebacterium diphtheriae

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
UDP-alpha-D-galactopyranose Corynebacterium diphtheriae
-
UDP-alpha-D-galactofuranose
-
r

Organism

Organism UniProt Comment Textmining
Corynebacterium diphtheriae Q6NER4
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant expression of His6-tagged or GSG-tagged enzyme by nickel affinity chromatography and gel filtration Corynebacterium diphtheriae

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
UDP-alpha-D-galactopyranose
-
Corynebacterium diphtheriae UDP-alpha-D-galactofuranose
-
r

Subunits

Subunits Comment Organism
More structure of dimeric recombinant GSG-CdUGM Corynebacterium diphtheriae

Synonyms

Synonyms Comment Organism
CdUGM
-
Corynebacterium diphtheriae
Glf
-
Corynebacterium diphtheriae
UGM
-
Corynebacterium diphtheriae

Cofactor

Cofactor Comment Organism Structure
FAD tightly bound to the enzyme Corynebacterium diphtheriae

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0049
-
2-((4-(3,4-dichlorophenyl)thiazol-2-yl)amino)-3-(4-iodophenyl)propanoic acid pH 7.0, temperature not specified in the publication Corynebacterium diphtheriae

General Information

General Information Comment Organism
additional information active site structure, the citrate ion forms salt bridges with UGM residues R288 and H290 and numerous ordered water molecules, thereby participating in a hydrogen-bonding network with the active site residues. A strong density feature is observed bridging the citrate ion and the oxidized FAD Corynebacterium diphtheriae