Cloned (Comment) | Organism |
---|---|
expressed in Escherichia coli DH10B | Escherichia coli |
Protein Variants | Comment | Organism |
---|---|---|
D66A | site-saturation mutagenesis at position 66, 8fold increase in minimum inhibitory concentration for ceftazidime compared with the wild type (0.25 to 2 microg/ml). Mutation results in only minor changes in steady-state protein levels | Escherichia coli |
D66C | site-saturation mutagenesis at position 66. Expression of this variant is diminished relative to that of the other proteins | Escherichia coli |
D66L | site-saturation mutagenesis at position 66, rise in resistance against ceftazidime compared with the wild type | Escherichia coli |
D66M | site-saturation mutagenesis at position 66, rise in resistance against ceftazidime compared with the wild type. Mutation results in only minor changes in steady-state protein levels | Escherichia coli |
D66N | site-saturation mutagenesis at position 66, mutation leads to a moderate enhancement of extended-spectrum cephalosporin resistance and an increase in cefepime and cefotaxime resistance. Mutation results in only minor changes in steady-state protein levels | Escherichia coli |
D66P | site-saturation mutagenesis at position 66 | Escherichia coli |
D66W | site-saturation mutagenesis at position 66, mutation results in only minor changes in steady-state protein levels | Escherichia coli |
D66Y | site-saturation mutagenesis at position 66, mutation results in only minor changes in steady-state protein levels | Escherichia coli |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
ampicillin | - |
Escherichia coli |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.002 | - |
(6R,7S)-3-[(3-carboxy-4-nitro-phenyl)sulfanylmethyl]-8-oxo-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo-[4.2.0]-oct-2-ene-2-carboxylic acid | D66N mutant, pH 7.4, room temperature | Escherichia coli | |
0.0024 | - |
(6R,7S)-3-[(3-carboxy-4-nitro-phenyl)sulfanylmethyl]-8-oxo-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo-[4.2.0]-oct-2-ene-2-carboxylic acid | wild type, pH 7.4, room temperature | Escherichia coli | |
0.0027 | - |
ampicillin | D66Y mutant, pH 7.4, room temperature | Escherichia coli | |
0.0032 | - |
(6R,7S)-3-[(3-carboxy-4-nitro-phenyl)sulfanylmethyl]-8-oxo-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo-[4.2.0]-oct-2-ene-2-carboxylic acid | D66M mutant, pH 7.4, room temperature | Escherichia coli | |
0.006 | - |
ampicillin | D66A mutant, pH 7.4, room temperature | Escherichia coli | |
0.006 | - |
(6R,7S)-3-[(3-carboxy-4-nitro-phenyl)sulfanylmethyl]-8-oxo-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo-[4.2.0]-oct-2-ene-2-carboxylic acid | D66W mutant, pH 7.4, room temperature | Escherichia coli | |
0.007 | - |
(6R,7S)-3-[(3-carboxy-4-nitro-phenyl)sulfanylmethyl]-8-oxo-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo-[4.2.0]-oct-2-ene-2-carboxylic acid | D66Y mutant, pH 7.4, room temperature | Escherichia coli | |
0.009 | - |
cephalothin | wild type, pH 7.4, room temperature | Escherichia coli | |
0.01 | - |
cephalothin | D66M mutant, pH 7.4, room temperature | Escherichia coli | |
0.011 | - |
cephalothin | D66N mutant, pH 7.4, room temperature | Escherichia coli | |
0.012 | - |
ampicillin | D66M mutant, pH 7.4, room temperature | Escherichia coli | |
0.013 | - |
(6R,7S)-3-[(3-carboxy-4-nitro-phenyl)sulfanylmethyl]-8-oxo-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo-[4.2.0]-oct-2-ene-2-carboxylic acid | D66A mutant, pH 7.4, room temperature | Escherichia coli | |
0.014 | - |
cefotaxime | wild type OXA-1, pH 7.4, room temperature | Escherichia coli | |
0.021 | - |
ampicillin | D66W mutant, pH 7.4, room temperature | Escherichia coli | |
0.021 | - |
cefotaxime | His6-tagged wild type OXA-1, pH 7.4, room temperature | Escherichia coli | |
0.021 | - |
ampicillin | wild type, pH 7.4, room temperature | Escherichia coli | |
0.023 | - |
ampicillin | D66N mutant, pH 7.4, room temperature | Escherichia coli | |
0.024 | - |
cefotaxime | D66N mutant, pH 7.4, room temperature | Escherichia coli | |
0.027 | - |
cefepime | D66A mutant, pH 7.4, room temperature | Escherichia coli | |
0.029 | - |
ampicillin | wild type OXA-1, pH 7.4, room temperature | Escherichia coli | |
0.035 | - |
cefepime | D66M mutant, pH 7.4, room temperature | Escherichia coli | |
0.036 | - |
cefotaxime | D66M mutant, pH 7.4, room temperature | Escherichia coli | |
0.036 | - |
ampicillin | His6-tagged wild type OXA-1, pH 7.4, room temperature | Escherichia coli | |
0.036 | - |
cefotaxime | wild type, pH 7.4, room temperature | Escherichia coli | |
0.037 | - |
cephalothin | D66Y mutant, pH 7.4, room temperature | Escherichia coli | |
0.057 | - |
cefotaxime | D66Y mutant, pH 7.4, room temperature | Escherichia coli | |
0.059 | - |
cephalothin | D66W mutant, pH 7.4, room temperature | Escherichia coli | |
0.07 | - |
cefotaxime | D66A mutant, pH 7.4, room temperature | Escherichia coli | |
0.1 | - |
cephalothin | D66A mutant, pH 7.4, room temperature | Escherichia coli | |
0.15 | - |
cefepime | D66N mutant, pH 7.4, room temperature | Escherichia coli | |
0.17 | - |
cefepime | wild type, pH 7.4, room temperature | Escherichia coli | |
0.21 | - |
cefepime | D66W mutant, pH 7.4, room temperature | Escherichia coli | |
0.23 | - |
cefepime | D66Y mutant, pH 7.4, room temperature | Escherichia coli |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Escherichia coli | P13661 | - |
- |
Purification (Comment) | Organism |
---|---|
wild type OXA-1 purified by CM-cellulose chromatography and His6-tagged wild type OXA-1 purified by nickel-affinity chromatography | Escherichia coli |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
(6R,7S)-3-[(3-carboxy-4-nitro-phenyl)sulfanylmethyl]-8-oxo-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo-[4.2.0]-oct-2-ene-2-carboxylic acid + H2O | - |
Escherichia coli | ? | - |
? | |
ampicillin + H2O | - |
Escherichia coli | (2R,4S)-2-[(R)-[[(2R)-2-amino-2-phenylacetyl]amino](carboxy)methyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid | - |
? | |
cefepime + H2O | - |
Escherichia coli | (2R)-2-[(R)-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino](carboxy)methyl]-5-[(1-methylpyrrolidinium-1-yl)methyl]-3,6-dihydro-2H-1,3-thiazine-4-carboxylate | - |
? | |
cefotaxime + H2O | - |
Escherichia coli | (2R)-5-[(acetyloxy)methyl]-2-[(R)-[[(2E)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino](carboxy)methyl]-3,6-dihydro-2H-1,3-thiazine-4-carboxylic acid | - |
? | |
cephalothin + H2O | - |
Escherichia coli | (2R)-5-[(acetyloxy)methyl]-2-[(R)-carboxy[(thiophen-2-ylacetyl)amino]methyl]-3,6-dihydro-2H-1,3-thiazine-4-carboxylic acid | - |
? |
Synonyms | Comment | Organism |
---|---|---|
beta-lactamase | - |
Escherichia coli |
OXA-1 | - |
Escherichia coli |
oxa-1 beta-lactamase | - |
Escherichia coli |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.008 | - |
cefepime | D66W mutant, pH 7.4, room temperature | Escherichia coli | |
0.08 | - |
(6R,7S)-3-[(3-carboxy-4-nitro-phenyl)sulfanylmethyl]-8-oxo-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo-[4.2.0]-oct-2-ene-2-carboxylic acid | D66W mutant, pH 7.4, room temperature | Escherichia coli | |
0.15 | - |
cephalothin | D66W mutant, pH 7.4, room temperature | Escherichia coli | |
0.17 | - |
(6R,7S)-3-[(3-carboxy-4-nitro-phenyl)sulfanylmethyl]-8-oxo-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo-[4.2.0]-oct-2-ene-2-carboxylic acid | D66M mutant, pH 7.4, room temperature | Escherichia coli | |
0.19 | - |
(6R,7S)-3-[(3-carboxy-4-nitro-phenyl)sulfanylmethyl]-8-oxo-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo-[4.2.0]-oct-2-ene-2-carboxylic acid | D66A mutant, pH 7.4, room temperature | Escherichia coli | |
0.25 | - |
(6R,7S)-3-[(3-carboxy-4-nitro-phenyl)sulfanylmethyl]-8-oxo-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo-[4.2.0]-oct-2-ene-2-carboxylic acid | D66Y mutant, pH 7.4, room temperature | Escherichia coli | |
0.27 | - |
cephalothin | D66A mutant, pH 7.4, room temperature | Escherichia coli | |
0.28 | - |
cephalothin | D66Y mutant, pH 7.4, room temperature | Escherichia coli | |
0.31 | - |
cefotaxime | D66M mutant, pH 7.4, room temperature | Escherichia coli | |
0.37 | - |
cefotaxime | D66A mutant, pH 7.4, room temperature | Escherichia coli | |
0.38 | - |
cephalothin | D66M mutant, pH 7.4, room temperature | Escherichia coli | |
0.43 | - |
cefepime | D66M mutant, pH 7.4, room temperature | Escherichia coli | |
0.55 | - |
cefepime | D66A mutant, pH 7.4, room temperature | Escherichia coli | |
0.71 | - |
cefotaxime | D66Y mutant, pH 7.4, room temperature | Escherichia coli | |
1.2 | - |
(6R,7S)-3-[(3-carboxy-4-nitro-phenyl)sulfanylmethyl]-8-oxo-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo-[4.2.0]-oct-2-ene-2-carboxylic acid | D66N mutant, pH 7.4, room temperature | Escherichia coli | |
1.6 | - |
cephalothin | D66N mutant, pH 7.4, room temperature | Escherichia coli | |
1.6 | - |
(6R,7S)-3-[(3-carboxy-4-nitro-phenyl)sulfanylmethyl]-8-oxo-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo-[4.2.0]-oct-2-ene-2-carboxylic acid | wild type, pH 7.4, room temperature | Escherichia coli | |
2.7 | - |
cephalothin | wild type, pH 7.4, room temperature | Escherichia coli | |
3.5 | - |
cefotaxime | D66N mutant, pH 7.4, room temperature | Escherichia coli | |
3.8 | - |
cefepime | D66Y mutant, pH 7.4, room temperature | Escherichia coli | |
5.3 | - |
ampicillin | His6-tagged wild type OXA-1, pH 7.4, room temperature | Escherichia coli | |
5.3 | - |
cefotaxime | wild type, pH 7.4, room temperature | Escherichia coli | |
6.7 | - |
ampicillin | wild type OXA-1, pH 7.4, room temperature | Escherichia coli | |
10.6 | - |
ampicillin | D66Y mutant, pH 7.4, room temperature | Escherichia coli | |
13 | - |
ampicillin | D66A mutant, pH 7.4, room temperature | Escherichia coli | |
27 | - |
cefepime | D66N mutant, pH 7.4, room temperature | Escherichia coli | |
34 | - |
cefepime | wild type, pH 7.4, room temperature | Escherichia coli | |
43 | - |
ampicillin | D66M mutant, pH 7.4, room temperature | Escherichia coli | |
56 | - |
ampicillin | D66W mutant, pH 7.4, room temperature | Escherichia coli | |
440 | - |
cefotaxime | wild type OXA-1, pH 7.4, room temperature | Escherichia coli | |
480 | - |
ampicillin | D66N mutant, pH 7.4, room temperature | Escherichia coli | |
520 | - |
cefotaxime | His6-tagged wild type OXA-1, pH 7.4, room temperature | Escherichia coli | |
520 | - |
ampicillin | wild type, pH 7.4, room temperature | Escherichia coli |