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Literature summary for 2.7.1.190 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

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

KM Value [mM]

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Staphylococcus aureus P0A0C1
-
-

Substrates and Products (Substrate)

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

Synonyms

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

Turnover Number [1/s]

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

Ki Value [mM]

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

General Information

General Information Comment Organism
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]

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