Cloned (Comment) | Organism |
---|---|
expressed in Escherichia coli BL21(DE3) cells | Escherichia coli |
Crystallization (Comment) | Organism |
---|---|
in complex with inhibitor 4-(3-ethylthiophen-2-yl)benzene-1,2-diol, hanging drop vapour diffusion method, using 100 mM MES, pH 6.5, 2 mM MnCl2, and 17% PEG 20000 | Escherichia coli |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
4-(1,3-thiazol-2-yl)benzene-1,2-diol | does only inhibit Fe2+-activated MetAP enzyme, but not Mn2+- or Co2+-activated MetAP enzymes | Escherichia coli | |
4-(2,5-dichlorothiophen-3-yl)benzene-1,2-diol | - |
Escherichia coli | |
4-(2,5-dimethylthiophen-3-yl)benzene-1,2-diol | specific inhibition of Fe2+-loaded MetAP | Escherichia coli | |
4-(2-aminothiazol-4-yl)benzene-1,2-diol | specific inhibition of Fe2+-loaded MetAP | Escherichia coli | |
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol | does only inhibit Fe2+-activated MetAP enzyme, but not Mn2+- or Co2+-activated MetAP enzymes | Escherichia coli | |
4-(3-(2-bromoethyl)thiophen-2-yl)benzene-1,2-diol | - |
Escherichia coli | |
4-(3-butylthiophen-2-yl)benzene-1,2-diol | - |
Escherichia coli | |
4-(3-ethylthiophen-2-yl)benzene-1,2-diol | - |
Escherichia coli | |
4-(3-methylthiophen-2-yl)benzene-1,2-diol | - |
Escherichia coli | |
4-(3-propylthiophen-2-yl)benzene-1,2-diol | - |
Escherichia coli | |
4-(4-bromo-2,5-dimethylthiophen-3-yl)benzene-1,2-diol | - |
Escherichia coli | |
4-(5-chlorothiophen-2-yl)benzene-1,2-diol | - |
Escherichia coli | |
4-(5-methylthiophen-2-yl)benzene-1,2-diol | - |
Escherichia coli | |
4-(thiophen-2-yl)benzene-1,2-diol | - |
Escherichia coli | |
4-(thiophen-3-yl)benzene-1,2-diol | - |
Escherichia coli | |
5-(3,4-dihydroxyphenyl)-N-isopropyl-2-methylthiazole-4-carboxamide | specific inhibition of Fe2+-loaded MetAP | Escherichia coli | |
5-(3,4-dihydroxyphenyl)thiophene-2-carbonitrile | - |
Escherichia coli | |
cyclopropyl 5-(3,4-dihydroxyphenyl)-2-methyl-1,3-thiazole-4-carboxylate | - |
Escherichia coli | |
N-cyclopropyl-2-(3,4-dihydroxyphenyl)thiophene-3-carboxamide | specific inhibition of Fe2+-loaded MetAP | Escherichia coli | |
N-cyclopropyl-5-(3,4-dihydroxyphenyl)thiophene-2-carboxamide | - |
Escherichia coli |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Co2+ | - |
Escherichia coli | |
Fe2+ | Fe2+ is the likely metal cofactor used by MetAP in the cellular environment | Escherichia coli | |
Mn2+ | - |
Escherichia coli |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Escherichia coli | P0AE18 | - |
- |
Purification (Comment) | Organism |
---|---|
- |
Escherichia coli |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
L-Met-7-amido-4-methylcoumarin + H2O | - |
Escherichia coli | L-Met + 7-amino-4-methylcoumarin | - |
? |
Synonyms | Comment | Organism |
---|---|---|
MetAP | - |
Escherichia coli |
methionine aminopeptidase | - |
Escherichia coli |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0021 | - |
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2 | Escherichia coli | 4-(4-bromo-2,5-dimethylthiophen-3-yl)benzene-1,2-diol | |
0.0024 | - |
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2 | Escherichia coli | 4-(4-bromo-2,5-dimethylthiophen-3-yl)benzene-1,2-diol | |
0.0031 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | 4-(4-bromo-2,5-dimethylthiophen-3-yl)benzene-1,2-diol | |
0.0038 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 | Escherichia coli | 4-(thiophen-3-yl)benzene-1,2-diol | |
0.0051 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | 4-(thiophen-2-yl)benzene-1,2-diol | |
0.0066 | - |
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2 | Escherichia coli | 4-(2-aminothiazol-4-yl)benzene-1,2-diol | |
0.0066 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | 4-(2-aminothiazol-4-yl)benzene-1,2-diol | |
0.0073 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | 4-(3-(2-bromoethyl)thiophen-2-yl)benzene-1,2-diol | |
0.0074 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | 4-(2,5-dimethylthiophen-3-yl)benzene-1,2-diol | |
0.0078 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | N-cyclopropyl-2-(3,4-dihydroxyphenyl)thiophene-3-carboxamide | |
0.008 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | 4-(3-methylthiophen-2-yl)benzene-1,2-diol | |
0.0092 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | 4-(3-butylthiophen-2-yl)benzene-1,2-diol | |
0.0111 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | cyclopropyl 5-(3,4-dihydroxyphenyl)-2-methyl-1,3-thiazole-4-carboxylate | |
0.0128 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | 4-(5-chlorothiophen-2-yl)benzene-1,2-diol | |
0.0129 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | 4-(3-ethylthiophen-2-yl)benzene-1,2-diol | |
0.013 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | 4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol | |
0.014 | - |
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2 | Escherichia coli | 4-(3-(2-bromoethyl)thiophen-2-yl)benzene-1,2-diol | |
0.014 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | 4-(3-propylthiophen-2-yl)benzene-1,2-diol | |
0.0148 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | 5-(3,4-dihydroxyphenyl)thiophene-2-carbonitrile | |
0.0154 | - |
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2 | Escherichia coli | 5-(3,4-dihydroxyphenyl)-N-isopropyl-2-methylthiazole-4-carboxamide | |
0.0154 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | 5-(3,4-dihydroxyphenyl)-N-isopropyl-2-methylthiazole-4-carboxamide | |
0.0157 | - |
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2 | Escherichia coli | 4-(thiophen-2-yl)benzene-1,2-diol | |
0.0166 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | 4-(1,3-thiazol-2-yl)benzene-1,2-diol | |
0.0202 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | 4-(2,5-dichlorothiophen-3-yl)benzene-1,2-diol | |
0.0224 | - |
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2 | Escherichia coli | 4-(3-(2-bromoethyl)thiophen-2-yl)benzene-1,2-diol | |
0.023 | - |
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2 | Escherichia coli | 4-(3-methylthiophen-2-yl)benzene-1,2-diol | |
0.0237 | - |
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2 | Escherichia coli | 4-(thiophen-2-yl)benzene-1,2-diol | |
0.0238 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | N-cyclopropyl-5-(3,4-dihydroxyphenyl)thiophene-2-carboxamide | |
0.0275 | - |
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2 | Escherichia coli | 4-(thiophen-3-yl)benzene-1,2-diol | |
0.028 | - |
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2 | Escherichia coli | 4-(5-methylthiophen-2-yl)benzene-1,2-diol | |
0.0285 | - |
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2 | Escherichia coli | N-cyclopropyl-5-(3,4-dihydroxyphenyl)thiophene-2-carboxamide | |
0.0304 | - |
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2 | Escherichia coli | 5-(3,4-dihydroxyphenyl)thiophene-2-carbonitrile | |
0.0327 | - |
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid | Escherichia coli | 4-(5-methylthiophen-2-yl)benzene-1,2-diol | |
0.034 | - |
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2 | Escherichia coli | N-cyclopropyl-5-(3,4-dihydroxyphenyl)thiophene-2-carboxamide | |
0.0343 | - |
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2 | Escherichia coli | 4-(3-propylthiophen-2-yl)benzene-1,2-diol | |
0.0363 | - |
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2 | Escherichia coli | 5-(3,4-dihydroxyphenyl)thiophene-2-carbonitrile | |
0.0404 | - |
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2 | Escherichia coli | 4-(thiophen-3-yl)benzene-1,2-diol | |
0.0427 | - |
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2 | Escherichia coli | 4-(3-methylthiophen-2-yl)benzene-1,2-diol | |
0.0448 | - |
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2 | Escherichia coli | 4-(5-chlorothiophen-2-yl)benzene-1,2-diol | |
0.0482 | - |
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2 | Escherichia coli | 4-(3-butylthiophen-2-yl)benzene-1,2-diol | |
0.0486 | - |
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2 | Escherichia coli | 4-(2,5-dichlorothiophen-3-yl)benzene-1,2-diol | |
0.0515 | - |
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2 | Escherichia coli | 4-(5-methylthiophen-2-yl)benzene-1,2-diol | |
0.0557 | - |
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2 | Escherichia coli | 4-(3-ethylthiophen-2-yl)benzene-1,2-diol | |
0.0624 | - |
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2 | Escherichia coli | 4-(2,5-dichlorothiophen-3-yl)benzene-1,2-diol | |
0.0626 | - |
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2 | Escherichia coli | 4-(3-ethylthiophen-2-yl)benzene-1,2-diol | |
0.0923 | - |
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2 | Escherichia coli | cyclopropyl 5-(3,4-dihydroxyphenyl)-2-methyl-1,3-thiazole-4-carboxylate | |
0.1 | - |
IC50 above 0.1 mM, Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2 | Escherichia coli | N-cyclopropyl-2-(3,4-dihydroxyphenyl)thiophene-3-carboxamide | |
0.1 | - |
IC50 above 0.1 mM, Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2 | Escherichia coli | 4-(5-chlorothiophen-2-yl)benzene-1,2-diol | |
0.1 | - |
IC50 above 0.1 mM, Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2 | Escherichia coli | 4-(3-propylthiophen-2-yl)benzene-1,2-diol | |
0.1 | - |
IC50 above 0.1 mM, Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2 | Escherichia coli | 4-(3-butylthiophen-2-yl)benzene-1,2-diol | |
0.1 | - |
IC50 above 0.1 mM, Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2 | Escherichia coli | 4-(2,5-dimethylthiophen-3-yl)benzene-1,2-diol | |
0.1 | - |
IC50 above 0.1 mM, Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2 | Escherichia coli | N-cyclopropyl-2-(3,4-dihydroxyphenyl)thiophene-3-carboxamide | |
0.1 | - |
IC50 above 0.1 mM, Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2 | Escherichia coli | 4-(2,5-dimethylthiophen-3-yl)benzene-1,2-diol | |
0.1 | - |
IC50 above 0.1 mM, Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2 | Escherichia coli | 4-(2-aminothiazol-4-yl)benzene-1,2-diol | |
0.1 | - |
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2 | Escherichia coli | cyclopropyl 5-(3,4-dihydroxyphenyl)-2-methyl-1,3-thiazole-4-carboxylate | |
0.1 | - |
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2 | Escherichia coli | 5-(3,4-dihydroxyphenyl)-N-isopropyl-2-methylthiazole-4-carboxamide |