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Literature summary extracted from

  • Norris, A.L.; Ozen, C.; Serpersu, E.H.
    Thermodynamics and kinetics of association of antibiotics with the aminoglycoside acetyltransferase (3)-IIIb, a resistance-causing enzyme (2010), Biochemistry, 49, 4027-4035.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.3.1.81 expression in Escherichia coli Pseudomonas aeruginosa

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.81 kanamycin A substrate inhibition Pseudomonas aeruginosa
2.3.1.81 kanamycin B substrate inhibition Pseudomonas aeruginosa
2.3.1.81 additional information only small aminoglycosides without intraring constraints show substrate inhibition Pseudomonas aeruginosa
2.3.1.81 ribostamycin substrate inhibition Pseudomonas aeruginosa
2.3.1.81 tobramycin substrate inhibition Pseudomonas aeruginosa

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.3.1.81 0.0012
-
 neomycin B pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 0.0013
-
 tobramycin pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 0.0015
-
 sisomycin pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 0.0023
-
 ribostamycin pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 0.0026
-
 kanamycin B pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 0.0033
-
 paromomycin pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 0.0036
-
 lividomycin A pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 0.0048
-
 kanamycin A pH 7.6, 25°C Pseudomonas aeruginosa

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.81 Pseudomonas aeruginosa
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.81 acetyl-CoA + kanamycin A
-
 Pseudomonas aeruginosa CoA + N3'-acetylkanamycin A
-
 ?
2.3.1.81 acetyl-CoA + kanamycin B
-
 Pseudomonas aeruginosa CoA + N3'-acetylkanamycin B
-
 ?
2.3.1.81 acetyl-CoA + lividomycin A
-
 Pseudomonas aeruginosa CoA + ?
-
 ?
2.3.1.81 acetyl-CoA + neomycin B
-
 Pseudomonas aeruginosa CoA + N3-acetyl-neomycin B
-
 ?
2.3.1.81 acetyl-CoA + paromomycin
-
 Pseudomonas aeruginosa CoA + N3'-acetyl-paromomycin
-
 ?
2.3.1.81 acetyl-CoA + ribostamycin
-
 Pseudomonas aeruginosa CoA + ?
-
 ?
2.3.1.81 acetyl-CoA + sisomycin
-
 Pseudomonas aeruginosa CoA + N3'-acetylsisomycin
-
 ?
2.3.1.81 acetyl-CoA + tobramycin
-
 Pseudomonas aeruginosa CoA + N3'-acetyltobramycin
-
 ?
2.3.1.81 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

EC Number Synonyms Comment Organism
2.3.1.81 AAC (3)-IIIb
-
 Pseudomonas aeruginosa

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.3.1.81 9.5
-
 neomycin B pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 23.5
-
 ribostamycin pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 33.6
-
 paromomycin pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 33.8
-
 lividomycin A pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 46.3
-
 sisomycin pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 47.8
-
 tobramycin pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 51.4
-
 kanamycin A pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 54.5
-
 kanamycin B pH 7.6, 25°C Pseudomonas aeruginosa

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.3.1.81 0.0059
-
 ribostamycin pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 0.381
-
 kanamycin A pH 7.6, 25°C Pseudomonas aeruginosa

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
2.3.1.81 9100
-
 neomycin B pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 9500
-
 lividomycin A pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 10600
-
 ribostamycin pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 10800
-
 paromomycin pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 11200
-
 kanamycin A pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 33400
-
 sisomycin pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 34400
-
 kanamycin B pH 7.6, 25°C Pseudomonas aeruginosa
2.3.1.81 60500
-
 tobramycin pH 7.6, 25°C Pseudomonas aeruginosa