Cloned (Comment) | Organism |
---|---|
- |
Vibrio cholerae serotype O1 |
Protein Variants | Comment | Organism |
---|---|---|
E144C | mutation in subunit NrqB, the inhibitory effects of and 3-[(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-dien-1-yl]-2-methylquinolin-4(1H)-one 2-azido-5-iodobenzoate are almost completely abolished, while their the binding reactivities are unchanged | Vibrio cholerae serotype O1 |
G140A | mutation in subunit NrqB, the inhibitory effects of 5-azido-3-[(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-dien-1-yl]-2-methylquinolin-4(1H)-one 4-iodobenzoate and 3-[(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-dien-1-yl]-2-methylquinolin-4(1H)-one 2-azido-5-iodobenzoate are almost completely abolished, while their the binding reactivities are unchanged | Vibrio cholerae serotype O1 |
G141A | mutation in subunit NrqB, decrease in the inhibitory effects of koromicin and 3-[(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-dien-1-yl]-2-methylquinolin-4(1H)-one 2-azido-5-iodobenzoate | Vibrio cholerae serotype O1 |
G38V | mutation in subunit NrqA, no significant changes in the effects of inhibitors tested | Vibrio cholerae serotype O1 |
Y36A | mutation in subunit NrqA, no significant changes in the effects of inhibitors tested | Vibrio cholerae serotype O1 |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-n-heptyl-4-hydroxyquinoline N-oxide | - |
Vibrio cholerae serotype O1 | |
3-[(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-dien-1-yl]-2-methylquinolin-4(1H)-one 2-azido-5-iodobenzoate | - |
Vibrio cholerae serotype O1 | |
5-azido-3-[(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-dien-1-yl]-2-methylquinolin-4(1H)-one 4-iodobenzoate | - |
Vibrio cholerae serotype O1 | |
aurachin D-42 | the quinolone ring and alkyl side chain of inhibitor aurachin bind to the NqrB subunit in the regions Arg-43-Lys-54 and Trp-23-Gly-89, respectively | Vibrio cholerae serotype O1 | |
korormicin | - |
Vibrio cholerae serotype O1 |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Vibrio cholerae serotype O1 | Q9KPS1 and Q9KPS2 and P0C6E0 and Q9X4Q6 and Q9X4Q7 and Q9X4Q8 | Q9KPS1: subunit NqrA, Q9KPS2: subunit NqrB, P0C6E0: subunit NqrC, Q9X4Q6: subunit NqrD, Q9X4Q7: subunit NqrE, Q9X4Q8: subunit NqrF. The enzyme consists of six subunits encoded by the NQR operon. | - |
Vibrio cholerae serotype O1 ATCC 39315 | Q9KPS1 and Q9KPS2 and P0C6E0 and Q9X4Q6 and Q9X4Q7 and Q9X4Q8 | Q9KPS1: subunit NqrA, Q9KPS2: subunit NqrB, P0C6E0: subunit NqrC, Q9X4Q6: subunit NqrD, Q9X4Q7: subunit NqrE, Q9X4Q8: subunit NqrF. The enzyme consists of six subunits encoded by the NQR operon. | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | the ubiquinone ring binds to the NqrA subunit in the regions Leu-32-Met-39 and Phe-131-Lys-138, encompassing the rear wall of a predicted ubiquinone-binding cavity. The binding sites for ubiquinone and aurachin-type inhibitors are in close proximity but do not overlap one another | Vibrio cholerae serotype O1 | ? | - |
? | |
additional information | the ubiquinone ring binds to the NqrA subunit in the regions Leu-32-Met-39 and Phe-131-Lys-138, encompassing the rear wall of a predicted ubiquinone-binding cavity. The binding sites for ubiquinone and aurachin-type inhibitors are in close proximity but do not overlap one another | Vibrio cholerae serotype O1 ATCC 39315 | ? | - |
? |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000013 | - |
mutant G141A, pH 8.0, 30°C | Vibrio cholerae serotype O1 | 3-[(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-dien-1-yl]-2-methylquinolin-4(1H)-one 2-azido-5-iodobenzoate | |
0.0000016 | - |
wild-type, pH 8.0, 30°C | Vibrio cholerae serotype O1 | 3-[(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-dien-1-yl]-2-methylquinolin-4(1H)-one 2-azido-5-iodobenzoate | |
0.000002 | - |
wild-type, pH 8.0, 30°C | Vibrio cholerae serotype O1 | aurachin D-42 | |
0.0000027 | - |
mutant Y36A, pH 8.0, 30°C | Vibrio cholerae serotype O1 | aurachin D-42 | |
0.0000028 | - |
mutant G38V, pH 8.0, 30°C | Vibrio cholerae serotype O1 | aurachin D-42 | |
0.0000033 | - |
mutant G141A, pH 8.0, 30°C | Vibrio cholerae serotype O1 | aurachin D-42 | |
0.0000033 | - |
mutant Y36A, pH 8.0, 30°C | Vibrio cholerae serotype O1 | 3-[(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-dien-1-yl]-2-methylquinolin-4(1H)-one 2-azido-5-iodobenzoate | |
0.000005 | - |
wild-type, pH 8.0, 30°C | Vibrio cholerae serotype O1 | korormicin | |
0.0000057 | - |
mutant G38V, pH 8.0, 30°C | Vibrio cholerae serotype O1 | 3-[(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-dien-1-yl]-2-methylquinolin-4(1H)-one 2-azido-5-iodobenzoate | |
0.000008 | - |
mutant G38V, pH 8.0, 30°C | Vibrio cholerae serotype O1 | korormicin | |
0.0000081 | - |
mutant Y36A, pH 8.0, 30°C | Vibrio cholerae serotype O1 | korormicin | |
0.00001 | - |
mutant E144C, pH 8.0, 30°C | Vibrio cholerae serotype O1 | 3-[(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-dien-1-yl]-2-methylquinolin-4(1H)-one 2-azido-5-iodobenzoate | |
0.00059 | - |
wild-type, pH 8.0, 30°C | Vibrio cholerae serotype O1 | 5-azido-3-[(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-dien-1-yl]-2-methylquinolin-4(1H)-one 4-iodobenzoate | |
0.00082 | - |
mutant G141A, pH 8.0, 30°C | Vibrio cholerae serotype O1 | korormicin | |
0.00083 | - |
mutant Y36A, pH 8.0, 30°C | Vibrio cholerae serotype O1 | 5-azido-3-[(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-dien-1-yl]-2-methylquinolin-4(1H)-one 4-iodobenzoate | |
0.00096 | - |
mutant G38V, pH 8.0, 30°C | Vibrio cholerae serotype O1 | 5-azido-3-[(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-dien-1-yl]-2-methylquinolin-4(1H)-one 4-iodobenzoate | |
0.0012 | - |
mutant G141A, pH 8.0, 30°C | Vibrio cholerae serotype O1 | 2-n-heptyl-4-hydroxyquinoline N-oxide | |
0.002 | - |
wild-type, pH 8.0, 30°C | Vibrio cholerae serotype O1 | 2-n-heptyl-4-hydroxyquinoline N-oxide | |
0.0031 | - |
mutant Y36A, pH 8.0, 30°C | Vibrio cholerae serotype O1 | 2-n-heptyl-4-hydroxyquinoline N-oxide | |
0.0045 | - |
mutant G38V, pH 8.0, 30°C | Vibrio cholerae serotype O1 | 2-n-heptyl-4-hydroxyquinoline N-oxide | |
0.0052 | - |
mutant G141A, pH 8.0, 30°C | Vibrio cholerae serotype O1 | 5-azido-3-[(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-dien-1-yl]-2-methylquinolin-4(1H)-one 4-iodobenzoate | |
0.01 | - |
mutant G140A, pH 8.0, 30°C | Vibrio cholerae serotype O1 | 3-[(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-dien-1-yl]-2-methylquinolin-4(1H)-one 2-azido-5-iodobenzoate | |
0.012 | - |
mutant E144C, pH 8.0, 30°C | Vibrio cholerae serotype O1 | aurachin D-42 | |
0.012 | - |
mutant G140A, pH 8.0, 30°C | Vibrio cholerae serotype O1 | aurachin D-42 | |
0.027 | - |
mutant E144C, pH 8.0, 30°C | Vibrio cholerae serotype O1 | 5-azido-3-[(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-dien-1-yl]-2-methylquinolin-4(1H)-one 4-iodobenzoate | |
0.027 | - |
mutant G140A, pH 8.0, 30°C | Vibrio cholerae serotype O1 | 5-azido-3-[(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-dien-1-yl]-2-methylquinolin-4(1H)-one 4-iodobenzoate | |
0.05 | - |
mutant E144C, pH 8.0, 30°C | Vibrio cholerae serotype O1 | korormicin | |
0.05 | - |
mutant G140A, pH 8.0, 30°C | Vibrio cholerae serotype O1 | korormicin | |
0.2 | - |
mutant E144C, pH 8.0, 30°C | Vibrio cholerae serotype O1 | 2-n-heptyl-4-hydroxyquinoline N-oxide | |
0.2 | - |
mutant G140A, pH 8.0, 30°C | Vibrio cholerae serotype O1 | 2-n-heptyl-4-hydroxyquinoline N-oxide |