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Literature summary extracted from

  • Frase, H.; Toth, M.; Vakulenko, S.
    Revisiting the nucleotide and aminoglycoside substrate specificity of the bifunctional aminoglycoside acetyltransferase(6')-Ie/aminoglycoside phosphotransferase(2'')-Ia enzyme (2012), J. Biol. Chem., 287, 43262-43269.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.190 butirosin A/B
-
 Staphylococcus aureus
2.7.1.190 lividomycin A
-
 Staphylococcus aureus
2.7.1.190 neomycin B
-
 Staphylococcus aureus
2.7.1.190 paromomycin
-
 Staphylococcus aureus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.1.190 0.0003
-
 dibekacin pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 0.0008
-
 sisomicin pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 0.0008
-
 arbekacin pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 0.0041
-
 netilmicin pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 0.006
-
 gentamicin C pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 0.033
-
 amikacin pH 7.0, 22°C Staphylococcus aureus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.1.190 additional information Staphylococcus aureus GTP is the exclusive phosphate donor at intracellular nucleotide levels ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.190 Staphylococcus aureus P0A0C1
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.1.190 GTP + amikacin
-
 Staphylococcus aureus GDP + amikacin 2''-phosphate
-
 ?
2.7.1.190 GTP + arbekacin
-
 Staphylococcus aureus GDP + arbekacin 2''-phosphate
-
 ?
2.7.1.190 GTP + dibekacin
-
 Staphylococcus aureus GDP + dibekacin 2''-phosphate
-
 ?
2.7.1.190 GTP + gentamicin C
-
 Staphylococcus aureus GDP + gentamicin C 2''-phosphate
-
 ?
2.7.1.190 GTP + kanamycin A
-
 Staphylococcus aureus GDP + kanamycin A 2''-phosphate
-
 ?
2.7.1.190 GTP + kanamycin B
-
 Staphylococcus aureus GDP + kanamycin B 2''-phosphate
-
 ?
2.7.1.190 GTP + netilmicin
-
 Staphylococcus aureus GDP + netilmicin 2''-phosphate
-
 ?
2.7.1.190 GTP + sisomicin
-
 Staphylococcus aureus GDP + sisomicin 2''-phosphate
-
 ?
2.7.1.190 GTP + tobramycin
-
 Staphylococcus aureus GDP + tobramycin 2''-phosphate
-
 ?
2.7.1.190 additional information GTP is the exclusive phosphate donor at intracellular nucleotide levels Staphylococcus aureus ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.1.190 bifunctional aminoglycoside acetyltransferase(6')-Ie/aminoglycoside phosphotransferase(2'')-Ia
-
 Staphylococcus aureus

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.7.1.190 0.11
-
 tobramycin pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 0.12
-
 kanamycin B pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 0.15
-
 dibekacin pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 0.57
-
 kanamycin A pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 2.3
-
 arbekacin pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 3
-
 gentamicin C pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 3.7
-
 amikacin pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 6.5
-
 netilmicin pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 8.1
-
 sisomicin pH 7.0, 22°C Staphylococcus aureus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.7.1.190 0.00026
-
 neomycin B pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 0.0053
-
 paromomycin pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 0.011
-
 lividomycin A pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 0.14
-
 butirosin A/B pH 7.0, 22°C Staphylococcus aureus

General Information

EC Number General Information Comment Organism
2.7.1.190 physiological function enzyme phosphorylates 4,6-disubstituted aminoglycosides with high efficiency. Despite this proficiency, no resistance is conferred to some of these antibiotics by the enzyme in vivo. Phosphorylation of 4,5-disubstituted and atypical aminoglycosides are negligible and these antibiotics are not substrates. Instead, these aminoglycosides tend to stimulate an intrinsic GTPase activity of the enzyme Staphylococcus aureus

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
2.7.1.190 110
-
 amikacin pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 500
-
 dibekacin pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 2900
-
 arbekacin pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 5000
-
 gentamicin C pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 10000
-
 sisomicin pH 7.0, 22°C Staphylococcus aureus
2.7.1.190 16000
-
 netilmicin pH 7.0, 22°C Staphylococcus aureus