Cloned (Comment) | Organism |
---|---|
expressed in Novablue Escherichia coli cells | Trypanosoma brucei |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(3R,5S)-1-[(6-amino-9H-purin-9-yl)acetyl]-5-carbamoylpyrrolidin-3-yl L-lysylsulfamate | strong inhibitory effect | Trypanosoma brucei | |
(4R)-1-[(3-chloro-4-hydroxyphenyl)acetyl]-4-[(L-lysylsulfamoyl)oxy]-L-prolinamide | strong inhibitory effect | Trypanosoma brucei | |
(4S)-1-(3-bromo-4-hydroxybenzyl)-4-[hydroxy(L-lysyl)amino]-L-prolinamide | strong inhibitory effect | Trypanosoma brucei | |
additional information | the solid-phase combinatorial synthesis of a new library with potential inhibitory activity against the cytoplasmic lysyl-tRNA synthetase (LysRS) isoform of Trypanosoma brucei is described. Among the 65 compounds tested, there are 15 that have a mild inhibitory effect at 100 microM, and 3 have a strong effect | Trypanosoma brucei |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
cytoplasm | - |
Trypanosoma brucei | 5737 | - |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Trypanosoma brucei | Q580G3 | - |
- |
Purification (Comment) | Organism |
---|---|
nickel affinity column. All the products are purified in a Waters semipreparative HPLC system | Trypanosoma brucei |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + L-lysine + tRNALys | - |
Trypanosoma brucei | AMP + diphosphate + L-lysyl-tRNALys | - |
? |
Synonyms | Comment | Organism |
---|---|---|
LysRS | - |
Trypanosoma brucei |
Lysyl-tRNA synthetase | - |
Trypanosoma brucei |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00995 | - |
(4S)-1-(3-bromo-4-hydroxybenzyl)-4-[hydroxy(L-lysyl)amino]-L-prolinamide | - |
Trypanosoma brucei | |
0.02761 | - |
(3R,5S)-1-[(6-amino-9H-purin-9-yl)acetyl]-5-carbamoylpyrrolidin-3-yl L-lysylsulfamate | - |
Trypanosoma brucei | |
0.03442 | - |
(4R)-1-[(3-chloro-4-hydroxyphenyl)acetyl]-4-[(L-lysylsulfamoyl)oxy]-L-prolinamide | - |
Trypanosoma brucei |