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Literature summary for 3.5.2.6 extracted from
- Crystal structure and activity studies of the Mycobacterium tuberculosis beta-lactamase reveal its critical role in resistance to beta-lactam antibiotics (2006), Antimicrob. Agents Chemother., 50, 2762-2771.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expressed in Escherichia coli | Mycobacterium tuberculosis |
| plasmid pET28b is transformed into Escherichia coli BL21(DE3) | Mycobacterium tuberculosis |
Crystallization (Commentary)
| Crystallization (Comment) | Organism |
|---|---|
| hanging drop vapour diffusion method with 0.1 M Tris-HCl, pH 8.0, 2.0 M NH4H2PO4 | Mycobacterium tuberculosis |
| hanging-drop vapour-diffusion method, 1.2 A resolution | Mycobacterium tuberculosis |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| additional information | the amino acid substitutions N132G, R164A, R244A, and R276E explain the broad specificity of the enzyme, relatively low penicillinase activity, and resistance to clavulanic acid | Mycobacterium tuberculosis |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| clavulanate | - |
Mycobacterium tuberculosis |  |
| clavulanic acid | poor inhibitor | Mycobacterium tuberculosis | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.063 | - |
ampicillin | - |
Mycobacterium tuberculosis | |
| 0.063 | - |
ampicillin | at 30°C | Mycobacterium tuberculosis | |
| 0.117 | - |
cephalothin | - |
Mycobacterium tuberculosis | |
| 0.117 | - |
cephalothin | at 30°C | Mycobacterium tuberculosis | |
| 0.195 | - |
cefoxitin | - |
Mycobacterium tuberculosis | |
| 0.195 | - |
cefoxitin | at 30°C | Mycobacterium tuberculosis | |
| 0.279 | - |
meropenem | - |
Mycobacterium tuberculosis | |
| 0.279 | - |
meropenem | at 30°C | Mycobacterium tuberculosis | |
| 0.593 | - |
ceftazidime | - |
Mycobacterium tuberculosis | |
| 0.593 | - |
ceftazidime | at 30°C | Mycobacterium tuberculosis | |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 30630 | - |
truncated protein, matrix-assisted laser desorption ionization | Mycobacterium tuberculosis |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Mycobacterium tuberculosis | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
- |
Mycobacterium tuberculosis |
| Ni2+-loaded HiTrap chelating column chromatography and Superdex 200 gel filtration | Mycobacterium tuberculosis |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ampicillin + H2O | - |
Mycobacterium tuberculosis | (2R,4S)-2-[(R)-[[(2R)-2-amino-2-phenylacetyl]amino](carboxy)methyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid | - |
? | |
| ampicillin + H2O | low activity | Mycobacterium tuberculosis | (2R,4S)-2-[(R)-[[(2R)-2-amino-2-phenylacetyl]amino](carboxy)methyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid | - |
? | |
| cefoxitin + H2O | - |
Mycobacterium tuberculosis | (2R)-5-[(carbamoyloxy)methyl]-2-[(S)-carboxy(methoxy)[(thiophen-2-ylacetyl)amino]methyl]-3,6-dihydro-2H-1,3-thiazine-4-carboxylic acid | - |
? | |
| ceftazidime + H2O | - |
Mycobacterium tuberculosis | (2R)-2-[(R)-{[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-{[(2-carboxypropan-2-yl)oxy]imino}acetyl]amino}(carboxy)methyl]-5-[(pyridin-1-ium-1-yl)methyl]-3,6-dihydro-2H-1,3-thiazine-4-carboxylate | - |
? | |
| cephalothin + H2O | - |
Mycobacterium tuberculosis | (2R)-5-[(acetyloxy)methyl]-2-[(R)-carboxy[(thiophen-2-ylacetyl)amino]methyl]-3,6-dihydro-2H-1,3-thiazine-4-carboxylic acid | - |
? | |
| meropenem + H2O | - |
Mycobacterium tuberculosis | (4R,5S)-5-[(1S,2R)-1-carboxy-2-hydroxypropyl]-3-{[(3S,5S)-5-(dimethylcarbamoyl)pyrrolidin-3-yl]sulfanyl}-4-methyl-4,5-dihydro-1H-pyrrole-2-carboxylic acid | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| BlaC | - |
Mycobacterium tuberculosis |
| class A beta-lactamase | - |
Mycobacterium tuberculosis |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.2 | - |
ceftazidime | - |
Mycobacterium tuberculosis | |
| 0.2 | - |
ceftazidime | at 30°C | Mycobacterium tuberculosis | |
| 0.9 | - |
meropenem | - |
Mycobacterium tuberculosis | |
| 0.9 | - |
meropenem | at 30°C | Mycobacterium tuberculosis | |
| 1.1 | - |
cefoxitin | - |
Mycobacterium tuberculosis | |
| 1.1 | - |
cefoxitin | at 30°C | Mycobacterium tuberculosis | |
| 12.1 | - |
cephalothin | - |
Mycobacterium tuberculosis | |
| 12.1 | - |
cephalothin | at 30°C | Mycobacterium tuberculosis | |
| 18.5 | - |
ampicillin | - |
Mycobacterium tuberculosis | |
| 18.5 | - |
ampicillin | at 30°C | Mycobacterium tuberculosis | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0024 | - |
clavulanic acid | - |
Mycobacterium tuberculosis | |
| 0.0024 | - |
clavulanate | - |
Mycobacterium tuberculosis | |
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