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Literature summary for 2.3.1.81 extracted from
- Thermodynamics and kinetics of association of antibiotics with the aminoglycoside acetyltransferase (3)-IIIb, a resistance-causing enzyme (2010), Biochemistry, 49, 4027-4035.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression in Escherichia coli | Pseudomonas aeruginosa |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| kanamycin A | substrate inhibition | Pseudomonas aeruginosa |  |
| kanamycin B | substrate inhibition | Pseudomonas aeruginosa | |
| additional information | only small aminoglycosides without intraring constraints show substrate inhibition | Pseudomonas aeruginosa | |
| ribostamycin | substrate inhibition | Pseudomonas aeruginosa | |
| tobramycin | substrate inhibition | Pseudomonas aeruginosa | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0012 | - |
neomycin B | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 0.0013 | - |
tobramycin | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 0.0015 | - |
sisomycin | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 0.0023 | - |
ribostamycin | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 0.0026 | - |
kanamycin B | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 0.0033 | - |
paromomycin | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 0.0036 | - |
lividomycin A | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 0.0048 | - |
kanamycin A | pH 7.6, 25°C | Pseudomonas aeruginosa | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Pseudomonas aeruginosa | - |
- |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| acetyl-CoA + kanamycin A | - |
Pseudomonas aeruginosa | CoA + N3'-acetylkanamycin A | - |
? | |
| acetyl-CoA + kanamycin B | - |
Pseudomonas aeruginosa | CoA + N3'-acetylkanamycin B | - |
? | |
| acetyl-CoA + lividomycin A | - |
Pseudomonas aeruginosa | CoA + ? | - |
? | |
| acetyl-CoA + neomycin B | - |
Pseudomonas aeruginosa | CoA + N3-acetyl-neomycin B | - |
? | |
| acetyl-CoA + paromomycin | - |
Pseudomonas aeruginosa | CoA + N3'-acetyl-paromomycin | - |
? | |
| acetyl-CoA + ribostamycin | - |
Pseudomonas aeruginosa | CoA + ? | - |
? | |
| acetyl-CoA + sisomycin | - |
Pseudomonas aeruginosa | CoA + N3'-acetylsisomycin | - |
? | |
| acetyl-CoA + tobramycin | - |
Pseudomonas aeruginosa | CoA + N3'-acetyltobramycin | - |
? | |
| additional information | enzyme displays molecular size-dependent stoichiometry where binding stoichiometries are 1.5-2.0 for small antibiotics and 1.0 for larger. Antibiotic-enzyme interaction occurs with a favorable enthalpy and a compensating unfavorable entropy. The presence of coenzyme A significantly increases the affinity of the antibioticthe enthalpy of binding becomes more favored by 1.7-10.0fold in the presence of the cosubstrate CoASH, while the entropy becomes 2.0-22.5fold less favored. The overall free energy change is still only 1.0-1.9 kcal/mol from binary to ternary for all antibiotics tested, similar to those for other aminoglycoside-modifying enzymes | Pseudomonas aeruginosa | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| AAC (3)-IIIb | - |
Pseudomonas aeruginosa |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 9.5 | - |
neomycin B | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 23.5 | - |
ribostamycin | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 33.6 | - |
paromomycin | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 33.8 | - |
lividomycin A | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 46.3 | - |
sisomycin | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 47.8 | - |
tobramycin | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 51.4 | - |
kanamycin A | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 54.5 | - |
kanamycin B | pH 7.6, 25°C | Pseudomonas aeruginosa | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0059 | - |
ribostamycin | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 0.381 | - |
kanamycin A | pH 7.6, 25°C | Pseudomonas aeruginosa | |
kcat/KM [mM/s]
| kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 9100 | - |
neomycin B | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 9500 | - |
lividomycin A | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 10600 | - |
ribostamycin | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 10800 | - |
paromomycin | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 11200 | - |
kanamycin A | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 33400 | - |
sisomycin | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 34400 | - |
kanamycin B | pH 7.6, 25°C | Pseudomonas aeruginosa | |
| 60500 | - |
tobramycin | pH 7.6, 25°C | Pseudomonas aeruginosa | |
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