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Literature summary extracted from

  • Farrera-Sinfreu, J.; Espanol, Y.; Geslain, R.; Guitart, T.; Albericio, F.; Ribas de Pouplana, L.; Royo, M.
    Solid-phase combinatorial synthesis of a lysyl-tRNA synthetase (LysRS) inhibitory library (2008), J. Comb. Chem., 10, 391-400.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
6.1.1.6 expressed in Novablue Escherichia coli cells Trypanosoma brucei

Inhibitors

EC Number Inhibitors Comment Organism Structure
6.1.1.6 (3R,5S)-1-[(6-amino-9H-purin-9-yl)acetyl]-5-carbamoylpyrrolidin-3-yl L-lysylsulfamate strong inhibitory effect Trypanosoma brucei
6.1.1.6 (4R)-1-[(3-chloro-4-hydroxyphenyl)acetyl]-4-[(L-lysylsulfamoyl)oxy]-L-prolinamide strong inhibitory effect Trypanosoma brucei
6.1.1.6 (4S)-1-(3-bromo-4-hydroxybenzyl)-4-[hydroxy(L-lysyl)amino]-L-prolinamide strong inhibitory effect Trypanosoma brucei
6.1.1.6 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

EC Number Localization Comment Organism GeneOntology No. Textmining
6.1.1.6 cytoplasm
-
 Trypanosoma brucei 5737
-

Organism

EC Number Organism UniProt Comment Textmining
6.1.1.6 Trypanosoma brucei Q580G3
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
6.1.1.6 nickel affinity column. All the products are purified in a Waters semipreparative HPLC system Trypanosoma brucei

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
6.1.1.6 ATP + L-lysine + tRNALys
-
 Trypanosoma brucei AMP + diphosphate + L-lysyl-tRNALys
-
 ?

Synonyms

EC Number Synonyms Comment Organism
6.1.1.6 LysRS
-
 Trypanosoma brucei
6.1.1.6 Lysyl-tRNA synthetase
-
 Trypanosoma brucei

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
6.1.1.6 0.00995
-
 (4S)-1-(3-bromo-4-hydroxybenzyl)-4-[hydroxy(L-lysyl)amino]-L-prolinamide
-
 Trypanosoma brucei
6.1.1.6 0.02761
-
 (3R,5S)-1-[(6-amino-9H-purin-9-yl)acetyl]-5-carbamoylpyrrolidin-3-yl L-lysylsulfamate
-
 Trypanosoma brucei
6.1.1.6 0.03442
-
 (4R)-1-[(3-chloro-4-hydroxyphenyl)acetyl]-4-[(L-lysylsulfamoyl)oxy]-L-prolinamide
-
 Trypanosoma brucei