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Literature summary for 2.2.1.6 extracted from
- Characterization of acetohydroxyacid synthase from Mycobacterium tuberculosis and the identification of its new inhibitor from the screening of a chemical library (2005), FEBS Lett., 579, 4903-4910.
Application
| Application | Comment | Organism |
|---|---|---|
| pharmacology | AHAS might be a target protein for the development of anti-tuberculosis therapeutics | Mycobacterium tuberculosis |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| inducible overexpression of the His-tagged enzyme subunits in Escherichia coli strain BL21(DE3) | Mycobacterium tuberculosis |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| KHG20612 | inhibition kinetics and antimycobacterial activity, overview | Mycobacterium tuberculosis |  |
| additional information | screening of chemical libraries for effective inhibitors of the enzyme, overview | Mycobacterium tuberculosis | |
| pyrazosulfuron ethyl | IC50: 870 nM | Mycobacterium tuberculosis | |
| valine | - |
Mycobacterium tuberculosis | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | kinetics | Mycobacterium tuberculosis | |
| 1.56 | - |
pyruvate | pH 7.0, 37°C, holoenzyme | Mycobacterium tuberculosis | |
| 2.76 | - |
pyruvate | pH 7.0, 37°C, catalytic subunit | Mycobacterium tuberculosis | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | activates | Mycobacterium tuberculosis | |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 20400 | - |
x * 68300, recombinant His-tagged catalytic subunit, + x * 20400, recombinant His-tagged regulatory subunit, SDS-PAGE | Mycobacterium tuberculosis |
| 68300 | - |
x * 68300, recombinant His-tagged catalytic subunit, + x * 20400, recombinant His-tagged regulatory subunit, SDS-PAGE | Mycobacterium tuberculosis |
| 300000 | - |
above, recombinant holoenzyme, gel filtration | Mycobacterium tuberculosis |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| pyruvate | Mycobacterium tuberculosis | the enzyme catalyzes the first committed step in the biosynthesis of valine, leucine, and isoleucine | 2-acetolactate + CO2 | - |
? | |
| pyruvate | Mycobacterium tuberculosis H37Rv | the enzyme catalyzes the first committed step in the biosynthesis of valine, leucine, and isoleucine | 2-acetolactate + CO2 | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Mycobacterium tuberculosis | - |
- |
- |
| Mycobacterium tuberculosis H37Rv | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant His-tagged enzyme subunits from Escherichia coli to homogeneity by nickel affinity chromatography and dialysis | Mycobacterium tuberculosis |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| 2.8 | - |
purified catalytic subunit | Mycobacterium tuberculosis |
| 4.6 | - |
purified holoenzyme | Mycobacterium tuberculosis |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| pyruvate | - |
Mycobacterium tuberculosis | 2-acetolactate + CO2 | - |
? | |
| pyruvate | the enzyme catalyzes the first committed step in the biosynthesis of valine, leucine, and isoleucine | Mycobacterium tuberculosis | 2-acetolactate + CO2 | - |
? | |
| pyruvate | - |
Mycobacterium tuberculosis H37Rv | 2-acetolactate + CO2 | - |
? | |
| pyruvate | the enzyme catalyzes the first committed step in the biosynthesis of valine, leucine, and isoleucine | Mycobacterium tuberculosis H37Rv | 2-acetolactate + CO2 | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| oligomer | x * 68300, recombinant His-tagged catalytic subunit, + x * 20400, recombinant His-tagged regulatory subunit, SDS-PAGE | Mycobacterium tuberculosis |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| acetohydroxy acid synthase | - |
Mycobacterium tuberculosis |
| AHAS | - |
Mycobacterium tuberculosis |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Mycobacterium tuberculosis |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 6 | 8 | catalytic subunit | Mycobacterium tuberculosis |
| 7 | - |
holoenzyme | Mycobacterium tuberculosis |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| FAD | - |
Mycobacterium tuberculosis | |
| thiamine diphosphate | binding kinetics | Mycobacterium tuberculosis | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 16.3 | - |
valine | pH 7.0, 37°C, holoenzyme | Mycobacterium tuberculosis | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.00087 | - |
IC50: 870 nM | Mycobacterium tuberculosis | pyrazosulfuron ethyl | |
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