Cloned (Comment) | Organism |
---|---|
gene blaOXA-1, recombinant expression in Escerichia coli strain BL21(DE3) | Escherichia coli |
gene OXA24, recombinant expression in Escerichia coli strain BL21(DE3) | Acinetobacter baumannii |
Crystallization (Comment) | Organism |
---|---|
purified recombinant enzyme, hanging drop vapor diffusion method, mixing of 6 mg/ml protein in 10 mM HEPES, pH 7.5, with crystallization solution containing 0.1 M HEPES, pH 7.5, 0.1 M sodium acetate, and 28% PEG 2000, X-ray diffraction structure determination and analysis | Acinetobacter baumannii |
purified recombinant enzyme, hanging drop vapor diffusion method, mixing of 9 mg/ml protein solution with crystallization solution containing 0.05 M HEPES, pH 7.5, and 15% PEG 8000, X-ray diffraction structure determination and analysis | Escherichia coli |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
BRL 42715 | - |
Acinetobacter baumannii | |
BRL 42715 | - |
Escherichia coli | |
nitrocefin | substrate inhibition, NaHCO3 can reactivate the enzyme | Acinetobacter baumannii | |
penem 1 | a 6-methylidene penem, the carboxylated Lys84 in the active site of OXA-24 utilizes a catalytic water molecule to deacylate the Ser81, resulting in hydrolysis of the penem 1 inhibitor, and the enzyme is regenerated because Lys84 is not decarboxylated and hydrolyzes the next arriving inhibitor molecule, proposed mechanism for penem 1 and OXA-24, overview | Acinetobacter baumannii | |
penem 1 | a 6-methylidene penem, proposed mechanism for penem 1 and OXA-1, overview. Penem 1 can also cause the essentially irreversible decarboxylation of OXA-1 | Escherichia coli | |
penem 3 | a 6-methylidene penem | Acinetobacter baumannii | |
penem 3 | a 6-methylidene penem | Escherichia coli | |
SA-1-204 | a penam sulfone inhibitor, can effectively inhibit OXA-24 by decarboxylating the Lys84 in the active site | Acinetobacter baumannii | |
SA-1-204 | a penam sulfone inhibitor | Escherichia coli | |
tazobactam | - |
Acinetobacter baumannii | |
tazobactam | - |
Escherichia coli |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | steady-state kinetics | Escherichia coli | |
additional information | - |
additional information | steady-state kinetics | Acinetobacter baumannii | |
0.0083 | - |
nitrocefin | pH 7.2, temperature not specified in the publication, recombinant enzyme | Escherichia coli | |
0.028 | - |
nitrocefin | pH 7.2, temperature not specified in the publication, recombinant enzyme | Acinetobacter baumannii |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Acinetobacter baumannii | J9XTR7 | gene OXA24 | - |
Escherichia coli | P13661 | gene blaOXA-1 | - |
Reaction | Comment | Organism | Reaction ID |
---|---|---|---|
a beta-lactam + H2O = a substituted beta-amino acid | overall mechanism for beta-lactamase-inhibitor reaction, Quantum mechanical/molecular mechanical calculations and Raman spectral analysis, overview | Acinetobacter baumannii | |
a beta-lactam + H2O = a substituted beta-amino acid | overall mechanism for beta-lactamase-inhibitor reaction, Quantum mechanical/molecular mechanical calculations and Raman spectral analysis, overview. The protonation of the zeta-nitrogen leads to a barrierless decarboxylation of the lysine carbamate | Escherichia coli |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
(5R,6E)-6-[(4H,6H-pyrazolo[1,5-c][1,3]thiazol-2-yl)methylidene]-4-thia-1-azabicyclo[3.2.0]hept-2-en-7-one + H2O | - |
Acinetobacter baumannii | (2E)-2-[(2R)-2,3-dihydro-1,3-thiazol-2-yl]-3-(4H,6H-pyrazolo[1,5-c][1,3]thiazol-2-yl)prop-2-enoic acid | - |
? | |
(5R,6Z)-6-[(1,6,7,8a-tetrahydro-5H-imidazo[2,1-b][1,3]oxazin-2-yl)methylidene]-4-thia-1-azabicyclo[3.2.0]hept-2-en-7-one + H2O | - |
Acinetobacter baumannii | (2Z)-2-[(2R)-2,3-dihydro-1,3-thiazol-2-yl]-3-(1,6,7,8a-tetrahydro-5H-imidazo[2,1-b][1,3]oxazin-2-yl)prop-2-enoic acid | - |
? | |
nitrocefin + H2O | - |
Escherichia coli | (2R)-2-[(R)-carboxy[2-(thiophen-2-yl)acetamido]methyl]-5-[(E)-2-(2,4-dinitrophenyl)ethenyl]-3,6-dihydro-2H-1,3-thiazine-4-carboxylic acid | - |
? | |
nitrocefin + H2O | - |
Acinetobacter baumannii | (2R)-2-[(R)-carboxy[2-(thiophen-2-yl)acetamido]methyl]-5-[(E)-2-(2,4-dinitrophenyl)ethenyl]-3,6-dihydro-2H-1,3-thiazine-4-carboxylic acid | - |
? |
Synonyms | Comment | Organism |
---|---|---|
carbapenemase | UniProt | Acinetobacter baumannii |
class D beta-lactamase | - |
Escherichia coli |
class D beta-lactamase | - |
Acinetobacter baumannii |
OXA-1 | - |
Escherichia coli |
oxa-1 beta-lactamase | - |
Escherichia coli |
OXA-24 | - |
Acinetobacter baumannii |
OXA-24 beta-lactamase | - |
Acinetobacter baumannii |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.2 | - |
assay at | Escherichia coli |
7.2 | - |
assay at | Acinetobacter baumannii |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | inhibition kinetics | Escherichia coli | |
additional information | - |
additional information | inhibition kinetics | Acinetobacter baumannii | |
0.00003 | - |
penem 1 | pH 7.2, temperature not specified in the publication, recombinant enzyme | Acinetobacter baumannii | |
0.00005 | - |
penem 1 | pH 7.2, temperature not specified in the publication, recombinant enzyme | Escherichia coli | |
0.00015 | - |
penem 3 | pH 7.2, temperature not specified in the publication, recombinant enzyme | Acinetobacter baumannii | |
0.00038 | - |
penem 3 | pH 7.2, temperature not specified in the publication, recombinant enzyme | Escherichia coli |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00003 | - |
pH 7.2, temperature not specified in the publication, recombinant enzyme | Escherichia coli | penem 1 | |
0.00006 | - |
pH 7.2, temperature not specified in the publication, recombinant enzyme | Escherichia coli | penem 3 | |
0.00015 | - |
pH 7.2, temperature not specified in the publication, recombinant enzyme | Acinetobacter baumannii | penem 1 | |
0.00016 | - |
pH 7.2, temperature not specified in the publication, recombinant enzyme | Acinetobacter baumannii | penem 3 |