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Literature summary extracted from

  • Lee, T.; Verhey, T.; Antiperovitch, P.; Atamanyuk, D.; Desroy, N.; Oliveira, C.; Denis, A.; Gerusz, V.; Drocourt, E.; Loutet, S.; Hamad, M.; Stanetty, C.; Andres, S.; Sugiman-Marangos, S.; Kosma, P.; Valvano, M.; Moreau, F.; Junop, M.
    Structural-functional studies of Burkholderia cenocepacia D-glycero-beta-D-manno-heptose 7-phosphate kinase (HldA) and characterization of inhibitors with antibiotic adjuvant and antivirulence properties (2013), J. Med. Chem., 56, 1405-1417.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.1.167 expression in Escherichia coli Burkholderia cepacia

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.7.1.167 crystal structures of enzyme-substrate and enzyme-product complexes and complexes with inhibitors [[2-({[5-(2,6-dimethoxyphenyl)-1,2,4-triazin-3-yl]amino}methyl)-1,3-benzothiazol-5-yl]oxy]acetic acid and [[2-([[5-(2,6-dichlorophenyl)-1,2,4-triazin-3-yl]amino]methyl)-1,3-benzothiazol-5-yl]oxy]acetic acid. Enzyme HldA is structurally similar to members of the PfkB carbohydrate kinase family and appears to catalyze heptose phosphorylation via an in-line mechanism mediated mainly by a conserved aspartate, Asp270. Both inhibitors adopt a folded conformation and occupy the nucleotide-binding sites Burkholderia cepacia

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.167 [[2-([[5-(2,6-dichlorophenyl)-1,2,4-triazin-3-yl]amino]methyl)-1,3-benzothiazol-5-yl]oxy]acetic acid binds to the nucleotide-binding sites without altering the overall structure of the enzyme or interfering with the binding of D-glycero-beta-D-manno-heptose-7-phosphate Burkholderia cepacia
2.7.1.167 [[2-([[5-(2,6-dimethoxyphenyl)-1,2,4-triazin-3-yl]amino]methyl)-1,3-benzothiazol-5-yl]oxy]acetic acid binds to the nucleotide-binding sites without altering the overall structure of the enzyme or interfering with the binding of D-glycero-beta-D-manno-heptose-7-phosphate Burkholderia cepacia

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.167 Burkholderia cepacia B4EB35
-
-
2.7.1.167 Burkholderia cepacia J2315 B4EB35
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.1.167 D-glycero-beta-D-manno-heptose 7-phosphate + ATP
-
 Burkholderia cepacia D-glycero-beta-D-manno-heptose 1,7-bisphosphate + ADP
-
 ?
2.7.1.167 D-glycero-beta-D-manno-heptose 7-phosphate + ATP
-
 Burkholderia cepacia J2315 D-glycero-beta-D-manno-heptose 1,7-bisphosphate + ADP
-
 ?

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.1.167 0.00023
-
 pH not specified in the publication, temperature not specified in the publication Burkholderia cepacia [[2-([[5-(2,6-dichlorophenyl)-1,2,4-triazin-3-yl]amino]methyl)-1,3-benzothiazol-5-yl]oxy]acetic acid
2.7.1.167 0.00081
-
 pH not specified in the publication, temperature not specified in the publication Burkholderia cepacia [[2-([[5-(2,6-dimethoxyphenyl)-1,2,4-triazin-3-yl]amino]methyl)-1,3-benzothiazol-5-yl]oxy]acetic acid