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Literature summary for 2.3.1.82 extracted from

  • Draker, K.A.; Wright, G.D.
    Molecular mechanism of the enterococcal aminoglycoside 6'-N-acetyltransferase': role of GNAT-conserved residues in the chemistry of antibiotic inactivation (2004), Biochemistry, 43, 446-454.
    View publication on PubMed
Search for more literature for 2.3.1.82

Protein Variants

Protein Variants Comment Organism
E72A mutation causes a notable reduction in affinity for both the 4,5- and 4,5-disubstituted classes of aminoglycosides, with the largest changes being an 83fold decrease in the affinity for the minimal substrate neamine and a 175fold reduction in Km-value for kanamycin Enterococcus faecium
H74A kinetic parameters reveal only a small effect of the mutation on enzyme activity, Km-values for acetyl-CoA and the 4,5- and 4,6-disubstituted aminoglycosides only differs by a range of 2-7.5fold compared to that of the wild-type enzyme, indicating no significant change in apparent affinity Enterococcus faecium
L76A mutant enzyme shows virtually wild-type activity, with the biggest changes being a 3.6fold reduction in the apparent affinity for neomycin and a 3.7fold decrease in turnover number for amikacin Enterococcus faecium
L76P mutant enzyme is impaired in both aminoglycoside recognition and catalysis, 2300fold decrease in the ratio of turnover number to Kb-value for neamine, 1300fold reduction in the ratio of turnover number to Kb-value for tobramycin, no detectable activity towardskanamycin A and amikacin Enterococcus faecium
Y147A no detectable activity towardsamikacin Enterococcus faecium
Y147F decrease in aminoglycoside affinity ranges from a 6fold decrease for tobramycin to a large 170fold change in KM-value for amikacin Enterococcus faecium

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0033
-
 acetyl-CoA pH 6.0, 37°C, mutant enzyme L76A Enterococcus faecium
0.0041
-
 acetyl-CoA pH 6.0, 37°C, mutant enzyme Y147F Enterococcus faecium
0.0047
-
 acetyl-CoA pH 6.0, 37°C, mutant enzyme Y147A Enterococcus faecium
0.0053
-
 neomycin pH 6.0, 37°C, wild-type enzyme Enterococcus faecium
0.0058
-
 neamine pH 6.0, 37°C, wild-type enzyme Enterococcus faecium
0.0073
-
 acetyl-CoA pH 6.0, 37°C, mutant enzyme H74A Enterococcus faecium
0.0091
-
 ribostamycin pH 6.0, 37°C, wild-type enzyme Enterococcus faecium
0.0114
-
 amikacin pH 6.0, 37°C, mutant enzyme L76A Enterococcus faecium
0.0131
-
 amikacin pH 6.0, 37°C, wild-type enzyme Enterococcus faecium
0.0144
-
 kanamycin A pH 6.0, 37°C, mutant enzyme H74A Enterococcus faecium
0.0182
-
 neomycin pH 6.0, 37°C, mutant enzyme H74A Enterococcus faecium
0.019
-
 neomycin pH 6.0, 37°C, mutant enzyme L76A Enterococcus faecium
0.0199
-
 kanamycin A pH 6.0, 37°C, wild-type enzyme Enterococcus faecium
0.0214
-
 ribostamycin pH 6.0, 37°C, mutant enzyme L76A Enterococcus faecium
0.022
-
 tobramycin pH 6.0, 37°C, wild-type enzyme Enterococcus faecium
0.0224
-
 neamine pH 6.0, 37°C, mutant enzyme L76A Enterococcus faecium
0.0235
-
 acetyl-CoA pH 6.0, 37°C, wild-type enzyme Enterococcus faecium
0.0257
-
 kanamycin A pH 6.0, 37°C, mutant enzyme L76A Enterococcus faecium
0.029
-
 neomycin pH 6.0, 37°C, mutant enzyme E72A Enterococcus faecium
0.0369
-
 tobramycin pH 6.0, 37°C, mutant enzyme H74A Enterococcus faecium
0.0381
-
 ribostamycin pH 6.0, 37°C, mutant enzyme H74A Enterococcus faecium
0.0386
-
 neomycin pH 6.0, 37°C, mutant enzyme Y147A Enterococcus faecium
0.0432
-
 neamine pH 6.0, 37°C, mutant enzyme H74A Enterococcus faecium
0.0489
-
 acetyl-CoA pH 6.0, 37°C, mutant enzyme L76P Enterococcus faecium
0.0553
-
 neomycin pH 6.0, 37°C, mutant enzyme Y147F Enterococcus faecium
0.0573
-
 neomycin pH 6.0, 37°C, mutant enzyme L76P Enterococcus faecium
0.0582
-
 amikacin pH 6.0, 37°C, mutant enzyme H74A Enterococcus faecium
0.0682
-
 neamine pH 6.0, 37°C, mutant enzyme L76P Enterococcus faecium
0.107
-
 ribostamycin pH 6.0, 37°C, mutant enzyme L76P Enterococcus faecium
0.109
-
 ribostamycin pH 6.0, 37°C, mutant enzyme Y147A Enterococcus faecium
0.11
-
 kanamycin A pH 6.0, 37°C, mutant enzyme Y147A Enterococcus faecium
0.136
-
 tobramycin pH 6.0, 37°C, mutant enzyme Y147F Enterococcus faecium
0.146
-
 tobramycin pH 6.0, 37°C, mutant enzyme L76P Enterococcus faecium
0.147
-
 tobramycin pH 6.0, 37°C, mutant enzyme Y147A Enterococcus faecium
0.15
-
 neamine pH 6.0, 37°C, mutant enzyme Y147F Enterococcus faecium
0.154
-
 acetyl-CoA pH 6.0, 37°C, mutant enzyme E72A Enterococcus faecium
0.169
-
 neamine pH 6.0, 37°C, mutant enzyme Y147A Enterococcus faecium
0.301
-
 ribostamycin pH 6.0, 37°C, mutant enzyme E72A Enterococcus faecium
0.306
-
 ribostamycin pH 6.0, 37°C, mutant enzyme Y147F Enterococcus faecium
0.34
-
 kanamycin A pH 6.0, 37°C, mutant enzyme Y147F Enterococcus faecium
0.38
-
 amikacin pH 6.0, 37°C, mutant enzyme E72A Enterococcus faecium
0.482
-
 neamine pH 6.0, 37°C, mutant enzyme E72A Enterococcus faecium
0.62
-
 tobramycin pH 6.0, 37°C, mutant enzyme L76A Enterococcus faecium
1.15
-
 tobramycin pH 6.0, 37°C, mutant enzyme E72A Enterococcus faecium
2.19
-
 amikacin pH 6.0, 37°C, mutant enzyme Y147F Enterococcus faecium
3.49
-
 kanamycin A pH 6.0, 37°C, mutant enzyme E72A Enterococcus faecium

Organism

Organism UniProt Comment Textmining
Enterococcus faecium
-
 chromosomally encoded aminoglycoside 6'-N-acetyltransferase
-

Purification (Commentary)

Purification (Comment) Organism
-
 Enterococcus faecium

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-CoA + amikacin
-
 Enterococcus faecium CoA + N6'-acetylamikacin
-
 ?
acetyl-CoA + kanamycin A
-
 Enterococcus faecium CoA + N6'-acetylkanamycin A
-
 ?
acetyl-CoA + neamine
-
 Enterococcus faecium CoA + N6'-acetylneamine
-
 ?
acetyl-CoA + neomycin
-
 Enterococcus faecium CoA + N6'-acetylneomycin
-
 ?
acetyl-CoA + ribostamycin
-
 Enterococcus faecium CoA + N6'-acetylribostamycin
-
 ?
acetyl-CoA + tobramycin
-
 Enterococcus faecium CoA + N6'-acetyltobramycin
-
 ?

Synonyms

Synonyms Comment Organism
aminoglycoside 6'-N-acetyltransferase
-
 Enterococcus faecium

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.001
-
 neomycin pH 6.0, 37°C, mutant enzyme Y147A Enterococcus faecium
0.002
-
 neamine pH 6.0, 37°C, mutant enzyme L76P Enterococcus faecium
0.003
-
 amikacin pH 6.0, 37°C, mutant enzyme Y147F Enterococcus faecium
0.004
-
 tobramycin pH 6.0, 37°C, mutant enzyme Y147A Enterococcus faecium
0.004
-
 neamine pH 6.0, 37°C, mutant enzyme Y147A Enterococcus faecium
0.01
-
 tobramycin pH 6.0, 37°C, mutant enzyme L76P Enterococcus faecium
0.01
-
 ribostamycin pH 6.0, 37°C, mutant enzyme L76P Enterococcus faecium
0.01
-
 acetyl-CoA pH 6.0, 37°C, mutant enzyme Y147A Enterococcus faecium
0.01
-
 kanamycin A pH 6.0, 37°C, mutant enzyme Y147A Enterococcus faecium
0.02
-
 ribostamycin pH 6.0, 37°C, mutant enzyme Y147A Enterococcus faecium
0.03
-
 amikacin pH 6.0, 37°C, mutant enzyme L76A Enterococcus faecium
0.03
-
 kanamycin A pH 6.0, 37°C, mutant enzyme Y147F Enterococcus faecium
0.04
-
 amikacin pH 6.0, 37°C, mutant enzyme H74A Enterococcus faecium
0.04
-
 neomycin pH 6.0, 37°C, mutant enzyme L76P Enterococcus faecium
0.05
-
 amikacin pH 6.0, 37°C, mutant enzyme E72A Enterococcus faecium
0.05
-
 kanamycin A pH 6.0, 37°C, mutant enzyme H74A Enterococcus faecium
0.05
-
 neamine pH 6.0, 37°C, mutant enzyme Y147F Enterococcus faecium
0.06
-
 acetyl-CoA pH 6.0, 37°C, mutant enzyme L76P Enterococcus faecium
0.07
-
 acetyl-CoA pH 6.0, 37°C, mutant enzyme Y147F Enterococcus faecium
0.07
-
 neomycin pH 6.0, 37°C, mutant enzyme Y147F Enterococcus faecium
0.1
-
 tobramycin pH 6.0, 37°C, mutant enzyme Y147F Enterococcus faecium
0.11
-
 amikacin pH 6.0, 37°C, wild-type enzyme Enterococcus faecium
0.12
-
 ribostamycin pH 6.0, 37°C, mutant enzyme Y147F Enterococcus faecium
0.15
-
 neamine pH 6.0, 37°C, mutant enzyme H74A Enterococcus faecium
0.15
-
 ribostamycin pH 6.0, 37°C, mutant enzyme L76A Enterococcus faecium
0.16
-
 neomycin pH 6.0, 37°C, mutant enzyme L76A Enterococcus faecium
0.18
-
 acetyl-CoA pH 6.0, 37°C, mutant enzyme H74A Enterococcus faecium
0.19
-
 neomycin pH 6.0, 37°C, mutant enzyme H74A Enterococcus faecium
0.2
-
 neomycin pH 6.0, 37°C, wild-type enzyme Enterococcus faecium
0.23
-
 ribostamycin pH 6.0, 37°C, mutant enzyme H74A Enterococcus faecium
0.23
-
 acetyl-CoA pH 6.0, 37°C, mutant enzyme L76A Enterococcus faecium
0.27
-
 kanamycin A pH 6.0, 37°C, mutant enzyme L76A Enterococcus faecium
0.3
-
 tobramycin pH 6.0, 37°C, mutant enzyme H74A Enterococcus faecium
0.34
-
 ribostamycin pH 6.0, 37°C, wild-type enzyme Enterococcus faecium
0.35
-
 ribostamycin pH 6.0, 37°C, mutant enzyme E72A Enterococcus faecium
0.38
-
 neamine pH 6.0, 37°C, mutant enzyme L76A Enterococcus faecium
0.4
-
 acetyl-CoA pH 6.0, 37°C, wild-type enzyme Enterococcus faecium
0.42
-
 neamine pH 6.0, 37°C, wild-type enzyme Enterococcus faecium
0.44
-
 neamine pH 6.0, 37°C, mutant enzyme E72A Enterococcus faecium
0.55
-
 kanamycin A pH 6.0, 37°C, mutant enzyme E72A Enterococcus faecium
0.82
-
 kanamycin A pH 6.0, 37°C, wild-type enzyme Enterococcus faecium
0.89
-
 tobramycin pH 6.0, 37°C, mutant enzyme L76A Enterococcus faecium
0.99
-
 acetyl-CoA pH 6.0, 37°C, mutant enzyme E72A Enterococcus faecium
1.1
-
 tobramycin pH 6.0, 37°C, wild-type enzyme Enterococcus faecium
1.1
-
 tobramycin pH 6.0, 37°C, mutant enzyme E72A Enterococcus faecium
1.1
-
 neomycin pH 6.0, 37°C, mutant enzyme E72A Enterococcus faecium