Inhibitors | Comment | Organism | Structure |
---|---|---|---|
additional information | substrate inhibition, but not by tryptamine and 7,8-dichloro-1,2,3,4-tetrahydroisoquinoline | Oryctolagus cuniculus | |
N,N-Dimethyltryptamine | competitive inhibitor | Oryctolagus cuniculus |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.01 | - |
7,8-dichloro-1,2,3,4-tetrahydroisoquinoline | transferase A, pH 7.6 | Oryctolagus cuniculus | |
0.015 | - |
S-adenosyl-L-methionine | 1 mM tryptamine as methyl acceptor, pH 8.5 | Oryctolagus cuniculus | |
0.12 | - |
tryptamine | transferase B, pH 8.5 | Oryctolagus cuniculus | |
0.2 | - |
imidazole | transferase A, pH 8.5 | Oryctolagus cuniculus | |
0.24 | - |
desmethylimipramine | transferase B, pH 8.5 | Oryctolagus cuniculus | |
0.3 | - |
tryptamine | transferase A, pH 8.5 | Oryctolagus cuniculus | |
0.3 | - |
desmethylimipramine | transferase A, pH 8.5 | Oryctolagus cuniculus | |
1.5 | - |
pyrazole | transferase A, pH 7.6 | Oryctolagus cuniculus | |
2 | - |
7,8-dichloro-1,2,3,4-tetrahydroisoquinoline | transferase B, pH 7.6 | Oryctolagus cuniculus | |
3.2 | - |
pyrazole | transferase B, pH 7.6 | Oryctolagus cuniculus | |
5.1 | - |
imidazole | transferase B, pH 8.5 | Oryctolagus cuniculus | |
7.6 | - |
aniline | transferase A, pH 7.6 | Oryctolagus cuniculus | |
7.8 | - |
aniline | transferase B, pH 7.6 | Oryctolagus cuniculus |
Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
---|---|---|---|
additional information | - |
amino acid composition of transferase A | Oryctolagus cuniculus |
30000 | - |
gel filtration | Oryctolagus cuniculus |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
S-adenosyl-L-methionine + an amine | Oryctolagus cuniculus | enzymes participate in detoxication, recycling of drugs after initial demethylation | S-adenosyl-L-homocysteine + an N-methylamine | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Oryctolagus cuniculus | - |
amine N-methyltransferase A and B | - |
Oryctolagus cuniculus | - |
10-16 week old | - |
Oryctolagus cuniculus New Zealand | - |
10-16 week old | - |
Purification (Comment) | Organism |
---|---|
two N-methyltransferases A and B separable by ammonium sulfate fractionation, HPLC-ion exchange chromatography | Oryctolagus cuniculus |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
liver | two amine N-methyltransferases, A and B | Oryctolagus cuniculus | - |
Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
---|---|---|---|
0.000068 | - |
N-methyltransferase A, aniline | Oryctolagus cuniculus |
0.00022 | - |
N-methyltransferase B, desmethylimipramine | Oryctolagus cuniculus |
0.00026 | - |
N-methyltransferase A, desmethylimipramine | Oryctolagus cuniculus |
0.00044 | - |
N-methyltransferase A, tryptamine | Oryctolagus cuniculus |
0.00127 | - |
N-methyltransferase B, aniline | Oryctolagus cuniculus |
0.0031 | - |
N-methyltransferase B, tryptamine | Oryctolagus cuniculus |
Storage Stability | Organism |
---|---|
-80°C, partially purified, per month, less than 10% loss of activity | Oryctolagus cuniculus |
-80°C, purified, per month, about 25% loss of activity | Oryctolagus cuniculus |
2°C, per week, 25% loss of activity | Oryctolagus cuniculus |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | two N-methyltransferases A and B with very broad but overlapping substrate specificity for primary and secondary amines, lipophilic substrates, overview poor substrates, no substrates: N-acetylserotonine, 4-aminoacetophenone, 4-aminophenol, benzamide, 4-chloroaniline, deoxyepinephrine, 1,4-diaminobutane, dopamine, 1-ethanol-2-amine, ethylenediamine, histamine, histidine methylester, 3-hydroxytryptamine, indole, pyrrole, methylamine, N-methyldopamine, nicotinamide, octopamine, phenylalanine, phenylethanolamine, theophylline, tryptophan, tyrosine, N,N-dimethyltryptamine | Oryctolagus cuniculus | ? | - |
? | |
additional information | two N-methyltransferases A and B with very broad but overlapping substrate specificity for primary and secondary amines, lipophilic substrates, overview poor substrates, no substrates: N-acetylserotonine, 4-aminoacetophenone, 4-aminophenol, benzamide, 4-chloroaniline, deoxyepinephrine, 1,4-diaminobutane, dopamine, 1-ethanol-2-amine, ethylenediamine, histamine, histidine methylester, 3-hydroxytryptamine, indole, pyrrole, methylamine, N-methyldopamine, nicotinamide, octopamine, phenylalanine, phenylethanolamine, theophylline, tryptophan, tyrosine, N,N-dimethyltryptamine | Oryctolagus cuniculus New Zealand | ? | - |
? | |
S-adenosyl-L-methionine + 5-methyloxytryptamine | higher activity with transferase A | Oryctolagus cuniculus | ? | - |
? | |
S-adenosyl-L-methionine + 7,8-dichloro-1,2,3,4-tetrahydroisoquinoline | substrate with highest apparent kcat | Oryctolagus cuniculus | ? | - |
? | |
S-adenosyl-L-methionine + alpha-N-methyltryptamine | - |
Oryctolagus cuniculus | S-adenosyl-L-homocysteine + alpha,alpha-N,N-dimethyltryptamine | - |
? | |
S-adenosyl-L-methionine + alpha-N-methyltryptamine | - |
Oryctolagus cuniculus New Zealand | S-adenosyl-L-homocysteine + alpha,alpha-N,N-dimethyltryptamine | - |
? | |
S-adenosyl-L-methionine + an amine | enzymes participate in detoxication, recycling of drugs after initial demethylation | Oryctolagus cuniculus | S-adenosyl-L-homocysteine + an N-methylamine | - |
? | |
S-adenosyl-L-methionine + aniline | poor substrate | Oryctolagus cuniculus | S-adenosyl-L-homocysteine + N-methylaniline | - |
? | |
S-adenosyl-L-methionine + anisidine | higher activity with transferase B | Oryctolagus cuniculus | ? | - |
? | |
S-adenosyl-L-methionine + desmethylimipramine | higher activity with transferase A | Oryctolagus cuniculus | S-adenosyl-L-homocysteine + imipramine | - |
? | |
S-adenosyl-L-methionine + desmethylimipramine | higher activity with transferase A | Oryctolagus cuniculus New Zealand | S-adenosyl-L-homocysteine + imipramine | - |
? | |
S-adenosyl-L-methionine + imidazole | higher activity with transferase A | Oryctolagus cuniculus | ? | - |
? | |
S-adenosyl-L-methionine + N-methylbutylamine | only transferase A | Oryctolagus cuniculus | S-adenosyl-L-homocysteine + N,N-dimethylbutylamine | - |
? | |
S-adenosyl-L-methionine + N-methylcyclohexylamine | only transferase A | Oryctolagus cuniculus | S-adenosyl-L-homocysteine + N,N-dimethylcyclohexylamine | - |
? | |
S-adenosyl-L-methionine + N-methyltryptamine | - |
Oryctolagus cuniculus | S-adenosyl-L-homocysteine + N,N-dimethyltryptamine | - |
? | |
S-adenosyl-L-methionine + N-methyltryptamine | - |
Oryctolagus cuniculus New Zealand | S-adenosyl-L-homocysteine + N,N-dimethyltryptamine | - |
? | |
S-adenosyl-L-methionine + phenyltetrahydropyridine | higher activity with transferase A | Oryctolagus cuniculus | ? | - |
? | |
S-adenosyl-L-methionine + pyrazole | higher activity with transferase A | Oryctolagus cuniculus | ? | - |
? | |
S-adenosyl-L-methionine + tryptamine | i.e. 3-[2-aminoethyl] indole, best substrate, two N-methyltransferases: A and B, non-specific | Oryctolagus cuniculus | S-adenosyl-L-homocysteine + alpha-N-methyltryptamine | - |
? | |
S-adenosyl-L-methionine + tryptamine | i.e. 3-[2-aminoethyl] indole, best substrate, two N-methyltransferases: A and B, non-specific | Oryctolagus cuniculus New Zealand | S-adenosyl-L-homocysteine + alpha-N-methyltryptamine | - |
? |
Subunits | Comment | Organism |
---|---|---|
monomer | 1 * 30000, SDS-PAGE | Oryctolagus cuniculus |
More | aggregation upon denaturation leads to 60 kDa and 90 kDa fractions | Oryctolagus cuniculus |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Oryctolagus cuniculus |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0333 | - |
desmethylimipramine | transferase B, pH 8.5 | Oryctolagus cuniculus | |
0.0333 | - |
aniline | transferase A, pH 7.6 | Oryctolagus cuniculus | |
0.0833 | - |
imidazole | transferase A, pH 8.5 | Oryctolagus cuniculus | |
0.1 | - |
pyrazole | transferase B, pH 7.6 | Oryctolagus cuniculus | |
0.117 | - |
S-adenosyl-L-methionine | transferase B, pH 8.5 | Oryctolagus cuniculus | |
0.167 | - |
imidazole | transferase B, pH 8.5 | Oryctolagus cuniculus | |
0.2 | - |
S-adenosyl-L-methionine | transferase A, pH 8.5 | Oryctolagus cuniculus | |
0.233 | - |
desmethylimipramine | transferase A, pH 8.5 | Oryctolagus cuniculus | |
0.25 | - |
pyrazole | transferase A, pH 7.6 | Oryctolagus cuniculus | |
0.367 | - |
aniline | transferase B, pH 7.6 | Oryctolagus cuniculus | |
0.4 | - |
tryptamine | transferase A, pH 8.5 | Oryctolagus cuniculus | |
0.45 | - |
tryptamine | transferase B, pH 8.5 | Oryctolagus cuniculus | |
0.667 | - |
7,8-dichloro-1,2,3,4-tetrahydroisoquinoline | transferase A, pH 7.6 | Oryctolagus cuniculus | |
3.67 | - |
7,8-dichloro-1,2,3,4-tetrahydroisoquinoline | transferase B, pH 7.6 | Oryctolagus cuniculus |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
additional information | - |
transferase A: pI 4.9, transferase B: pI 5.1 | Oryctolagus cuniculus |
8.5 | - |
- |
Oryctolagus cuniculus |
pH Minimum | pH Maximum | Comment | Organism |
---|---|---|---|
7.2 | 8.9 | tryptamine, about half-maximal activity at pH 7.2 and 8.9, transferase A | Oryctolagus cuniculus |
7.5 | 8.8 | tryptamine, about half-maximal activity at pH 7.5 and 90% at pH 8.8, transferase B | Oryctolagus cuniculus |
pH Stability | pH Stability Maximum | Comment | Organism |
---|---|---|---|
6.2 | - |
optimal for transferase A | Oryctolagus cuniculus |
7.8 | - |
optimal for transferase B | Oryctolagus cuniculus |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
S-adenosyl-L-methionine | - |
Oryctolagus cuniculus |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.006 | - |
N,N-Dimethyltryptamine | N-methyltransferase B | Oryctolagus cuniculus | |
0.01 | - |
N,N-Dimethyltryptamine | N-methyltransferase A | Oryctolagus cuniculus |