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Literature summary for 2.7.1.189 extracted from
- Targeting quorum sensing high-throughput screening to identify novel LsrK inhibitors (2019), Int. J. Mol. Sci., 20, 3112 .
Application
| Application | Comment | Organism |
|---|---|---|
| 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)
| Cloned (Comment) | Organism |
|---|---|
| gene lsrK, recombinant overexpresison of His-tagged enzyme in Escherichia coli strain MET1158 | Salmonella enterica subsp. enterica serovar Typhimurium |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 7-deacetoxy-7-oxokhivorin | - |
Salmonella enterica subsp. enterica serovar Typhimurium |  |
| 7-dehydroxypryogallin-4-carboxylic acid | - |
Salmonella enterica subsp. enterica serovar Typhimurium | |
| acetyl isogambogic acid | - |
Salmonella enterica subsp. enterica serovar Typhimurium | |
| Agaric acid | - |
Salmonella enterica subsp. enterica serovar Typhimurium | |
| Aurin tricarboxylic acid | - |
Salmonella enterica subsp. enterica serovar Typhimurium | |
| celastrol | - |
Salmonella enterica subsp. enterica serovar Typhimurium | |
| fumarprotocetraric acid | - |
Salmonella enterica subsp. enterica serovar Typhimurium | |
| harpagoside | - |
Salmonella enterica subsp. enterica serovar Typhimurium | |
| additional information | poor inhibition by aurin tricarboxylic acid | Salmonella enterica subsp. enterica serovar Typhimurium | |
| protoporphyrin IX | - |
Salmonella enterica subsp. enterica serovar Typhimurium | |
| 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 | |
| stictic acid | - |
Salmonella enterica subsp. enterica serovar Typhimurium | |
| tetrachloroisophtalonitrile | - |
Salmonella enterica subsp. enterica serovar Typhimurium | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | required | Salmonella enterica subsp. enterica serovar Typhimurium | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + (S)-4,5-dihydroxypentane-2,3-dione | Salmonella enterica subsp. enterica serovar Typhimurium | - |
ADP + (S)-4-hydroxypentane-2,3-dione 5-phosphate | - |
? | |
| ATP + (S)-4,5-dihydroxypentane-2,3-dione | Salmonella enterica subsp. enterica serovar Typhimurium SGSC1412 | - |
ADP + (S)-4-hydroxypentane-2,3-dione 5-phosphate | - |
? | |
| 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
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Salmonella enterica subsp. enterica serovar Typhimurium | Q8ZKQ6 | - |
- |
| Salmonella enterica subsp. enterica serovar Typhimurium ATCC 700720 | Q8ZKQ6 | - |
- |
| Salmonella enterica subsp. enterica serovar Typhimurium SGSC1412 | Q8ZKQ6 | - |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| 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)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + (S)-4,5-dihydroxypentane-2,3-dione | - |
Salmonella enterica subsp. enterica serovar Typhimurium | ADP + (S)-4-hydroxypentane-2,3-dione 5-phosphate | - |
? | |
| ATP + (S)-4,5-dihydroxypentane-2,3-dione | - |
Salmonella enterica subsp. enterica serovar Typhimurium SGSC1412 | ADP + (S)-4-hydroxypentane-2,3-dione 5-phosphate | - |
? | |
| 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
| Synonyms | Comment | Organism |
|---|---|---|
| lsrK | - |
Salmonella enterica subsp. enterica serovar Typhimurium |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 22 | - |
assay at room temperature | Salmonella enterica subsp. enterica serovar Typhimurium |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.1 | 7.4 | assay at | Salmonella enterica subsp. enterica serovar Typhimurium |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Salmonella enterica subsp. enterica serovar Typhimurium | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.001 | - |
pH 7.4, 22°C, recombinant enzyme | Salmonella enterica subsp. enterica serovar Typhimurium | Aurin tricarboxylic acid | |
| 0.001 | - |
pH 7.4, 22°C, recombinant enzyme | Salmonella enterica subsp. enterica serovar Typhimurium | rosolic acid | |
| 0.003 | - |
pH 7.4, 22°C, recombinant enzyme | Salmonella enterica subsp. enterica serovar Typhimurium | 7-deacetoxy-7-oxokhivorin | |
| 0.003 | - |
pH 7.4, 22°C, recombinant enzyme | Salmonella enterica subsp. enterica serovar Typhimurium | stictic acid | |
| 0.004 | - |
pH 7.4, 22°C, recombinant enzyme | Salmonella enterica subsp. enterica serovar Typhimurium | celastrol | |
| 0.004 | - |
pH 7.4, 22°C, recombinant enzyme | Salmonella enterica subsp. enterica serovar Typhimurium | acetyl isogambogic acid | |
| 0.007 | - |
pH 7.4, 22°C, recombinant enzyme | Salmonella enterica subsp. enterica serovar Typhimurium | Agaric acid | |
| 0.007 | - |
pH 7.4, 22°C, recombinant enzyme | Salmonella enterica subsp. enterica serovar Typhimurium | 7-dehydroxypryogallin-4-carboxylic acid | |
| 0.007 | - |
pH 7.4, 22°C, recombinant enzyme | Salmonella enterica subsp. enterica serovar Typhimurium | fumarprotocetraric acid | |
| 0.009 | - |
pH 7.4, 22°C, recombinant enzyme | Salmonella enterica subsp. enterica serovar Typhimurium | protoporphyrin IX | |
| 0.009 | - |
pH 7.4, 22°C, recombinant enzyme | Salmonella enterica subsp. enterica serovar Typhimurium | tetrachloroisophtalonitrile | |
| 0.01 | - |
pH 7.4, 22°C, recombinant enzyme | Salmonella enterica subsp. enterica serovar Typhimurium | harpagoside | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| malfunction | inhibition of LsrK impairs the quorum-sensing cascade and consequently reduces bacterial pathogenicity | Salmonella enterica subsp. enterica serovar Typhimurium |
| 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 |
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Release 2023.1 (January 2023)
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