Protein Variants | Comment | Organism |
---|---|---|
Q202W/G210S | less sensitive to N-((2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl)-4-((4-(morpholinomethyl)phenyl)ethynyl)benzamide than wild-type, that is inhibited about 75% by 4 nM N-((2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl)-4-((4-(morpholinomethyl)phenyl)ethynyl)benzamide | Escherichia coli |
S214G | completely inhibited by 0.5 microM N-((2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl)-4-((4-(morpholinomethyl)phenyl)ethynyl)benzamide, wild-type under the same conditions 50% inhibited | Rhizobium leguminosarum |
T179A | LpxC mutant is less sensitive to N-((2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl)-4-((4-(morpholinomethyl)phenyl)ethynyl)benzamide inhibition | Aquifex aeolicus |
W206Q/S214G | completely inhibited by 0.5 microM N-((2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl)-4-((4-(morpholinomethyl)phenyl)ethynyl)benzamide, wild-type under the same conditions 50% inhibited | Rhizobium leguminosarum |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(R)-3-(5,8-dihydronaphthalen-2-yl)-N-hydroxy-2-(naphthalene-2-sulfonamido)propanamide | - |
Escherichia coli | |
(R)-3-(5,8-dihydronaphthalen-2-yl)-N-hydroxy-2-(naphthalene-2-sulfonamido)propanamide | - |
Rhizobium leguminosarum | |
(S)-N-(1-(2-(3,4-dimethoxy-5-propylphenyl)-4,5-dihydrooxazol-4-yl)vinyl)hydroxylamine | - |
Escherichia coli | |
(S)-N-(1-(2-(3,4-dimethoxy-5-propylphenyl)-4,5-dihydrooxazol-4-yl)vinyl)hydroxylamine | - |
Rhizobium leguminosarum | |
additional information | (S)-N-(1-(2-(3,4-dimethoxy-5-propylphenyl)-4,5-dihydrooxazol-4-yl)vinyl)hydroxylamine and (R)-3-(5,8-dihydronaphthalen-2-yl)-N-hydroxy-2-(naphthalene-2-sulfonamido)propanamide do not inhibit Aquifex aeolicus LpxC | Aquifex aeolicus | |
additional information | no evidence of time-dependent inhibition is observed in assays with either the wild-type or mutants | Rhizobium leguminosarum | |
N-((2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl)-4-((4-(morpholinomethyl)phenyl)ethynyl)benzamide | as effectively as ciprofloxacin or tobramycin | Aquifex aeolicus | |
N-((2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl)-4-((4-(morpholinomethyl)phenyl)ethynyl)benzamide | as effectively as ciprofloxacin or tobramycin | Escherichia coli | |
N-((2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl)-4-((4-(morpholinomethyl)phenyl)ethynyl)benzamide | wild-type is insensitive to N-((2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl)-4-((4-(morpholinomethyl)phenyl)ethynyl)benzamide | Rhizobium leguminosarum |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Aquifex aeolicus | O67648 | - |
- |
Escherichia coli | - |
- |
- |
Rhizobium leguminosarum | Q1ME43 | - |
- |
Synonyms | Comment | Organism |
---|---|---|
deacetylase LpxC | - |
Escherichia coli |
deacetylase LpxC | - |
Aquifex aeolicus |
deacetylase LpxC | - |
Rhizobium leguminosarum |
LpxC | - |
Escherichia coli |
LpxC | - |
Aquifex aeolicus |
LpxC | - |
Rhizobium leguminosarum |
UDP-3-O-(R-3-hydroxyacyl)-N-acetylglucosamine deacetylase | - |
Escherichia coli |
UDP-3-O-(R-3-hydroxyacyl)-N-acetylglucosamine deacetylase | - |
Aquifex aeolicus |
UDP-3-O-(R-3-hydroxyacyl)-N-acetylglucosamine deacetylase | - |
Rhizobium leguminosarum |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.000003 | - |
N-((2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl)-4-((4-(morpholinomethyl)phenyl)ethynyl)benzamide | W206Q/S214G mutant | Rhizobium leguminosarum | |
0.0000035 | - |
N-((2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl)-4-((4-(morpholinomethyl)phenyl)ethynyl)benzamide | S214G mutant | Rhizobium leguminosarum | |
0.000004 | - |
N-((2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl)-4-((4-(morpholinomethyl)phenyl)ethynyl)benzamide | wild-type | Escherichia coli | |
0.000005 | - |
N-((2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl)-4-((4-(morpholinomethyl)phenyl)ethynyl)benzamide | Q202W/G210S mutant | Escherichia coli | |
0.000053 | - |
(S)-N-(1-(2-(3,4-dimethoxy-5-propylphenyl)-4,5-dihydrooxazol-4-yl)vinyl)hydroxylamine | wild-type | Escherichia coli | |
0.000069 | - |
(R)-3-(5,8-dihydronaphthalen-2-yl)-N-hydroxy-2-(naphthalene-2-sulfonamido)propanamide | wild-type | Escherichia coli | |
0.000086 | - |
(R)-3-(5,8-dihydronaphthalen-2-yl)-N-hydroxy-2-(naphthalene-2-sulfonamido)propanamide | Q202W/G210S mutant | Escherichia coli | |
0.00034 | - |
N-((2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl)-4-((4-(morpholinomethyl)phenyl)ethynyl)benzamide | wild-type | Rhizobium leguminosarum | |
0.00034 | - |
(S)-N-(1-(2-(3,4-dimethoxy-5-propylphenyl)-4,5-dihydrooxazol-4-yl)vinyl)hydroxylamine | Q202W/G210S mutant | Escherichia coli | |
0.0007 | - |
(R)-3-(5,8-dihydronaphthalen-2-yl)-N-hydroxy-2-(naphthalene-2-sulfonamido)propanamide | W206Q/S214G mutant | Rhizobium leguminosarum | |
0.0058 | - |
(R)-3-(5,8-dihydronaphthalen-2-yl)-N-hydroxy-2-(naphthalene-2-sulfonamido)propanamide | wild-type | Rhizobium leguminosarum | |
0.11 | - |
(S)-N-(1-(2-(3,4-dimethoxy-5-propylphenyl)-4,5-dihydrooxazol-4-yl)vinyl)hydroxylamine | W206Q/S214G mutant | Rhizobium leguminosarum | |
0.38 | - |
(S)-N-(1-(2-(3,4-dimethoxy-5-propylphenyl)-4,5-dihydrooxazol-4-yl)vinyl)hydroxylamine | wild-type | Rhizobium leguminosarum |