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Literature summary extracted from

  • Gatta, V.; Ilina, P.; Porter, A.; McElroy, S.; Tammela, P.
    Targeting quorum sensing high-throughput screening to identify novel LsrK inhibitors (2019), Int. J. Mol. Sci., 20, 3112 .
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
2.7.1.189 drug development the enzyme is a target for inhibitor development to establish quorum-sensing inhibition, one of the most promising strategies to face the threat of bacterial resistance Salmonella enterica subsp. enterica serovar Typhimurium

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.1.189 gene lsrK, recombinant overexpresison of His-tagged enzyme in Escherichia coli strain MET1158 Salmonella enterica subsp. enterica serovar Typhimurium

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.189 7-deacetoxy-7-oxokhivorin
-
 Salmonella enterica subsp. enterica serovar Typhimurium
2.7.1.189 7-dehydroxypryogallin-4-carboxylic acid
-
 Salmonella enterica subsp. enterica serovar Typhimurium
2.7.1.189 acetyl isogambogic acid
-
 Salmonella enterica subsp. enterica serovar Typhimurium
2.7.1.189 Agaric acid
-
 Salmonella enterica subsp. enterica serovar Typhimurium
2.7.1.189 Aurin tricarboxylic acid
-
 Salmonella enterica subsp. enterica serovar Typhimurium
2.7.1.189 celastrol
-
 Salmonella enterica subsp. enterica serovar Typhimurium
2.7.1.189 fumarprotocetraric acid
-
 Salmonella enterica subsp. enterica serovar Typhimurium
2.7.1.189 harpagoside
-
 Salmonella enterica subsp. enterica serovar Typhimurium
2.7.1.189 additional information poor inhibition by aurin tricarboxylic acid Salmonella enterica subsp. enterica serovar Typhimurium
2.7.1.189 protoporphyrin IX
-
 Salmonella enterica subsp. enterica serovar Typhimurium
2.7.1.189 rosolic acid rosolic acid positively stabilizes His-LsrK in thermal shift at high concentrations, suggesting a low affnity binding interaction between the two, high target specificity Salmonella enterica subsp. enterica serovar Typhimurium
2.7.1.189 stictic acid
-
 Salmonella enterica subsp. enterica serovar Typhimurium
2.7.1.189 tetrachloroisophtalonitrile
-
 Salmonella enterica subsp. enterica serovar Typhimurium

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.1.189 Mg2+ required Salmonella enterica subsp. enterica serovar Typhimurium

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.1.189 ATP + (S)-4,5-dihydroxypentane-2,3-dione Salmonella enterica subsp. enterica serovar Typhimurium
-
 ADP + (S)-4-hydroxypentane-2,3-dione 5-phosphate
-
 ?
2.7.1.189 ATP + (S)-4,5-dihydroxypentane-2,3-dione Salmonella enterica subsp. enterica serovar Typhimurium SGSC1412
-
 ADP + (S)-4-hydroxypentane-2,3-dione 5-phosphate
-
 ?
2.7.1.189 ATP + (S)-4,5-dihydroxypentane-2,3-dione Salmonella enterica subsp. enterica serovar Typhimurium ATCC 700720
-
 ADP + (S)-4-hydroxypentane-2,3-dione 5-phosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.189 Salmonella enterica subsp. enterica serovar Typhimurium Q8ZKQ6
-
-
2.7.1.189 Salmonella enterica subsp. enterica serovar Typhimurium ATCC 700720 Q8ZKQ6
-
-
2.7.1.189 Salmonella enterica subsp. enterica serovar Typhimurium SGSC1412 Q8ZKQ6
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.1.189 recombinant His-tagged enzyme from Escherichia coli strain MET1158 by nickel affinity chromatography, and desalting gel filtration Salmonella enterica subsp. enterica serovar Typhimurium

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.1.189 ATP + (S)-4,5-dihydroxypentane-2,3-dione
-
 Salmonella enterica subsp. enterica serovar Typhimurium ADP + (S)-4-hydroxypentane-2,3-dione 5-phosphate
-
 ?
2.7.1.189 ATP + (S)-4,5-dihydroxypentane-2,3-dione
-
 Salmonella enterica subsp. enterica serovar Typhimurium SGSC1412 ADP + (S)-4-hydroxypentane-2,3-dione 5-phosphate
-
 ?
2.7.1.189 ATP + (S)-4,5-dihydroxypentane-2,3-dione
-
 Salmonella enterica subsp. enterica serovar Typhimurium ATCC 700720 ADP + (S)-4-hydroxypentane-2,3-dione 5-phosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.1.189 lsrK
-
 Salmonella enterica subsp. enterica serovar Typhimurium

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.1.189 22
-
 assay at room temperature Salmonella enterica subsp. enterica serovar Typhimurium

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.7.1.189 7.1 7.4 assay at Salmonella enterica subsp. enterica serovar Typhimurium

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.1.189 ATP
-
 Salmonella enterica subsp. enterica serovar Typhimurium

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.1.189 0.001
-
 pH 7.4, 22°C, recombinant enzyme Salmonella enterica subsp. enterica serovar Typhimurium Aurin tricarboxylic acid
2.7.1.189 0.001
-
 pH 7.4, 22°C, recombinant enzyme Salmonella enterica subsp. enterica serovar Typhimurium rosolic acid
2.7.1.189 0.003
-
 pH 7.4, 22°C, recombinant enzyme Salmonella enterica subsp. enterica serovar Typhimurium 7-deacetoxy-7-oxokhivorin
2.7.1.189 0.003
-
 pH 7.4, 22°C, recombinant enzyme Salmonella enterica subsp. enterica serovar Typhimurium stictic acid
2.7.1.189 0.004
-
 pH 7.4, 22°C, recombinant enzyme Salmonella enterica subsp. enterica serovar Typhimurium celastrol
2.7.1.189 0.004
-
 pH 7.4, 22°C, recombinant enzyme Salmonella enterica subsp. enterica serovar Typhimurium acetyl isogambogic acid
2.7.1.189 0.007
-
 pH 7.4, 22°C, recombinant enzyme Salmonella enterica subsp. enterica serovar Typhimurium Agaric acid
2.7.1.189 0.007
-
 pH 7.4, 22°C, recombinant enzyme Salmonella enterica subsp. enterica serovar Typhimurium 7-dehydroxypryogallin-4-carboxylic acid
2.7.1.189 0.007
-
 pH 7.4, 22°C, recombinant enzyme Salmonella enterica subsp. enterica serovar Typhimurium fumarprotocetraric acid
2.7.1.189 0.009
-
 pH 7.4, 22°C, recombinant enzyme Salmonella enterica subsp. enterica serovar Typhimurium protoporphyrin IX
2.7.1.189 0.009
-
 pH 7.4, 22°C, recombinant enzyme Salmonella enterica subsp. enterica serovar Typhimurium tetrachloroisophtalonitrile
2.7.1.189 0.01
-
 pH 7.4, 22°C, recombinant enzyme Salmonella enterica subsp. enterica serovar Typhimurium harpagoside

General Information

EC Number General Information Comment Organism
2.7.1.189 malfunction inhibition of LsrK impairs the quorum-sensing cascade and consequently reduces bacterial pathogenicity Salmonella enterica subsp. enterica serovar Typhimurium
2.7.1.189 physiological function LsrK is a kinase playing a key role in the processing of autoinducer-2 (AI-2), a quorum-sensing mediator in gut enteric bacteria Salmonella enterica subsp. enterica serovar Typhimurium