EC Number | Application | Comment | Organism |
---|---|---|---|
6.1.1.10 | drug development | parasite MetRS is an attractive drug target due to its essential role in protein synthesis and cell survival. Comparative sequence analysis discloses differences between the trypanosome and mammalian methionyl-tRNA synthetases | Trypanosoma brucei |
EC Number | Inhibitors | Comment | Organism | Structure |
---|---|---|---|---|
6.1.1.10 | 2-([3-[(2,3-dichlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one | 77.9% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-([3-[(2,4-dichlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one | 87.1% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-([3-[(2,5-dichlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one | 93.1% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-([3-[(2,6-dichlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one | 51.3% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-([3-[(2-chlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one | 31.8% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-([3-[(3,4-dichlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one | 91.7% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-([3-[(3,5-dibromo-2-ethoxybenzyl)amino]propyl]amino)quinolin-4(1H)-one | 98.2% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-([3-[(3,5-dibromo-2-methoxybenzyl)amino]propyl]amino)quinolin-4(1H)-one | 95.0% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-([3-[(3,5-dibromobenzyl)amino]propyl]amino)quinolin-4(1H)-one | 98.8% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-([3-[(3,5-dichlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one | 99.2% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-([3-[(3,5-difluorobenzyl)amino]propyl]amino)quinolin-4(1H)-one | 45.8% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-([3-[(3,5-dimethoxybenzyl)amino]propyl]amino)quinolin-4(1H)-one | 35.3% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-([3-[(3,5-dimethylbenzyl)amino]propyl]amino)quinolin-4(1H)-one | 91.1% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-([3-[(3-bromobenzyl)amino]propyl]amino)quinolin-4(1H)-one | 82.7% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-([3-[(3-chlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one | 97.3% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-([3-[(3-ethoxybenzyl)amino]propyl]amino)quinolin-4(1H)-one | 19.1% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-([3-[(4-chlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one | 52.0% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-[(3-[[3,5-bis(trifluoromethyl)benzyl]amino]propyl)amino]quinolin-4(1H)-one | 36.9% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-[(3-[[3-(trifluoromethoxy)benzyl]amino]propyl)amino]quinolin-4(1H)-one | 56.5% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 2-[[3-(benzylamino)propyl]amino]quinolin-4(1H)-one | 9.0% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | 3-[([3-[(4-oxo-1,4-dihydroquinolin-2-yl)amino]propyl]amino)methyl]benzonitrile | 20.2% inhibition at 50 nM | Trypanosoma brucei | |
6.1.1.10 | additional information | a homology model of the Trypanosoma brucei MetRS based on other MetRS structures is used to model binding of lead diaryl diamine compounds in the design and development of selective parasite MetRS inhibitors for treatment of African trypanosomiasis, overview | Trypanosoma brucei |
EC Number | Metals/Ions | Comment | Organism | Structure |
---|---|---|---|---|
6.1.1.10 | Mg2+ | required | Trypanosoma brucei |
EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
6.1.1.10 | ATP + L-methionine + tRNAMet | Trypanosoma brucei | - |
AMP + diphosphate + L-methionyl-tRNAMet | - |
? |
EC Number | Organism | UniProt | Comment | Textmining |
---|---|---|---|---|
6.1.1.10 | Trypanosoma brucei | - |
- |
- |
EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
6.1.1.10 | ATP + L-methionine + tRNAMet | - |
Trypanosoma brucei | AMP + diphosphate + L-methionyl-tRNAMet | - |
? |
EC Number | Subunits | Comment | Organism |
---|---|---|---|
6.1.1.10 | More | homology modeling and ligand docking studies of trypanosomatid MetRS enzymes, structure comparisons, overview | Trypanosoma brucei |
EC Number | Synonyms | Comment | Organism |
---|---|---|---|
6.1.1.10 | methionyl-tRNA synthetase | - |
Trypanosoma brucei |
6.1.1.10 | MetRS | - |
Trypanosoma brucei |
EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|---|
6.1.1.10 | 22 | - |
assay at room temperature | Trypanosoma brucei |
EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|---|
6.1.1.10 | 7.9 | - |
assay at | Trypanosoma brucei |
EC Number | Cofactor | Comment | Organism | Structure |
---|---|---|---|---|
6.1.1.10 | ATP | - |
Trypanosoma brucei |
EC Number | General Information | Comment | Organism |
---|---|---|---|
6.1.1.10 | metabolism | the single MetRS of Trypanosoma brucei is essential for normal cell growth | Trypanosoma brucei |