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Literature summary extracted from

  • Koh, C.Y.; Kim, J.E.; Wetzel, A.B.; de van der Schueren, W.J.; Shibata, S.; Ranade, R.M.; Liu, J.; Zhang, Z.; Gillespie, J.R.; Buckner, F.S.; Verlinde, C.L.; Fan, E.; Hol, W.G.
    Structures of Trypanosoma brucei methionyl-tRNA synthetase with urea-based inhibitors provide guidance for drug design against sleeping sickness (2014), PLoS Negl. Trop. Dis., 8, e2775 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
6.1.1.10 expressed in Escherichia coli Trypanosoma brucei

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
6.1.1.10 sitting drop vapor diffusion method, using 2.0-2.3 M (NH4)2SO4, 0.2 M NaCl and 0.1 M sodium cacodylate pH 6.2-6.8 Trypanosoma brucei

Inhibitors

EC Number Inhibitors Comment Organism Structure
6.1.1.10 N-(3-[[(2,5-dichlorothiophen-3-yl)methyl]amino]propyl)-N'-thiophen-3-ylurea
-
 Trypanosoma brucei
6.1.1.10 N-(3-[[(2-methyl-1-benzothiophen-3-yl)methyl]amino]propyl)-N'-thiophen-3-ylurea
-
 Trypanosoma brucei
6.1.1.10 N-(3-[[(3,5-dichlorophenyl)methyl]amino]propyl)-N'-(2-hydroxyphenyl)urea
-
 Trypanosoma brucei
6.1.1.10 N-(3-[[(3,5-dichlorophenyl)methyl]amino]propyl)-N'-(3-hydroxyphenyl)urea
-
 Trypanosoma brucei
6.1.1.10 N-(3-[[(3,5-dichlorophenyl)methyl]amino]propyl)-N'-phenylurea
-
 Trypanosoma brucei
6.1.1.10 N-(3-[[(3,5-dichlorophenyl)methyl]amino]propyl)-N'-thiophen-3-ylurea
-
 Trypanosoma brucei
6.1.1.10 N-(3-[[(3-chloro-5-methoxyphenyl)methyl]amino]propyl)-N'-phenylurea
-
 Trypanosoma brucei
6.1.1.10 N-(3-[[(3-chloro-5-methoxyphenyl)methyl]amino]propyl)-N'-thiophen-3-ylurea
-
 Trypanosoma brucei
6.1.1.10 N-(3-[[(3-cyanophenyl)methyl]amino]propyl)-N'-thiophen-3-ylurea
-
 Trypanosoma brucei
6.1.1.10 N-(3-[[(5-chloro-2-ethoxy-3-iodophenyl)methyl]amino]propyl)-N'-thiophen-3-ylurea
-
 Trypanosoma brucei
6.1.1.10 N-(3-[[(5-chloro-2-hydroxyphenyl)methyl]amino]propyl)-N'-thiophen-3-ylurea
-
 Trypanosoma brucei
6.1.1.10 N-[3-([[2-(benzyloxy)-5-chloro-3-(prop-2-en-1-yl)phenyl]methyl]amino)propyl]-N'-thiophen-3-ylurea
-
 Trypanosoma brucei
6.1.1.10 N-[3-([[5-chloro-2-hydroxy-3-(prop-2-en-1-yl)phenyl]methyl]amino)propyl]-N'-thiophen-3-ylurea
-
 Trypanosoma brucei
6.1.1.10 N-[3-[([5-chloro-3-(prop-2-en-1-yl)-2-[(prop-2-en-1-yl)oxy]phenyl]methyl)amino]propyl]-N'-thiophen-3-ylurea
-
 Trypanosoma brucei

Natural Substrates/ Products (Substrates)

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
-
 ?
6.1.1.10 ATP + L-methionine + tRNAMet Trypanosoma brucei 927
-
 AMP + diphosphate + L-methionyl-tRNAMet
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
6.1.1.10 Trypanosoma brucei Q38C91
-
-
6.1.1.10 Trypanosoma brucei 927 Q38C91
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
6.1.1.10 Ni-NTA column chromatography and Superdex 75 gel filtration Trypanosoma brucei

Substrates and Products (Substrate)

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
-
 ?
6.1.1.10 ATP + L-methionine + tRNAMet
-
 Trypanosoma brucei 927 AMP + diphosphate + L-methionyl-tRNAMet
-
 ?

Synonyms

EC Number Synonyms Comment Organism
6.1.1.10 methionyl-tRNA synthetase
-
 Trypanosoma brucei
6.1.1.10 MetRS
-
 Trypanosoma brucei

Cofactor

EC Number Cofactor Comment Organism Structure
6.1.1.10 ATP
-
 Trypanosoma brucei

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
6.1.1.10 0.000019
-
 pH and temperature not specified in the publication Trypanosoma brucei N-(3-[[(3-chloro-5-methoxyphenyl)methyl]amino]propyl)-N'-thiophen-3-ylurea
6.1.1.10 0.000028
-
 pH and temperature not specified in the publication Trypanosoma brucei N-(3-[[(3,5-dichlorophenyl)methyl]amino]propyl)-N'-thiophen-3-ylurea
6.1.1.10 0.000029
-
 pH and temperature not specified in the publication Trypanosoma brucei N-(3-[[(3,5-dichlorophenyl)methyl]amino]propyl)-N'-(3-hydroxyphenyl)urea
6.1.1.10 0.000039
-
 pH and temperature not specified in the publication Trypanosoma brucei N-(3-[[(3,5-dichlorophenyl)methyl]amino]propyl)-N'-(2-hydroxyphenyl)urea
6.1.1.10 0.000045
-
 pH and temperature not specified in the publication Trypanosoma brucei N-(3-[[(3-chloro-5-methoxyphenyl)methyl]amino]propyl)-N'-phenylurea
6.1.1.10 0.000057
-
 pH and temperature not specified in the publication Trypanosoma brucei N-(3-[[(3,5-dichlorophenyl)methyl]amino]propyl)-N'-phenylurea
6.1.1.10 0.000096
-
 pH and temperature not specified in the publication Trypanosoma brucei N-(3-[[(3-cyanophenyl)methyl]amino]propyl)-N'-thiophen-3-ylurea
6.1.1.10 0.000198
-
 pH and temperature not specified in the publication Trypanosoma brucei N-[3-([[5-chloro-2-hydroxy-3-(prop-2-en-1-yl)phenyl]methyl]amino)propyl]-N'-thiophen-3-ylurea
6.1.1.10 0.000316
-
 pH and temperature not specified in the publication Trypanosoma brucei N-(3-[[(5-chloro-2-hydroxyphenyl)methyl]amino]propyl)-N'-thiophen-3-ylurea
6.1.1.10 0.000324
-
 pH and temperature not specified in the publication Trypanosoma brucei N-(3-[[(2,5-dichlorothiophen-3-yl)methyl]amino]propyl)-N'-thiophen-3-ylurea
6.1.1.10 0.001231
-
 pH and temperature not specified in the publication Trypanosoma brucei N-[3-[([5-chloro-3-(prop-2-en-1-yl)-2-[(prop-2-en-1-yl)oxy]phenyl]methyl)amino]propyl]-N'-thiophen-3-ylurea
6.1.1.10 0.00136
-
 pH and temperature not specified in the publication Trypanosoma brucei N-(3-[[(2-methyl-1-benzothiophen-3-yl)methyl]amino]propyl)-N'-thiophen-3-ylurea
6.1.1.10 0.001678
-
 pH and temperature not specified in the publication Trypanosoma brucei N-[3-([[2-(benzyloxy)-5-chloro-3-(prop-2-en-1-yl)phenyl]methyl]amino)propyl]-N'-thiophen-3-ylurea
6.1.1.10 10
-
 IC50 above 10 mM, pH and temperature not specified in the publication Trypanosoma brucei N-(3-[[(5-chloro-2-ethoxy-3-iodophenyl)methyl]amino]propyl)-N'-thiophen-3-ylurea