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Literature summary for 6.1.1.10 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
Search for more literature for 6.1.1.10

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli Trypanosoma brucei

Crystallization (Commentary)

Crystallization (Comment) Organism
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

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + L-methionine + tRNAMet Trypanosoma brucei
-
 AMP + diphosphate + L-methionyl-tRNAMet
-
 ?
ATP + L-methionine + tRNAMet Trypanosoma brucei 927
-
 AMP + diphosphate + L-methionyl-tRNAMet
-
 ?

Organism

Organism UniProt Comment Textmining
Trypanosoma brucei Q38C91
-
-
Trypanosoma brucei 927 Q38C91
-
-

Purification (Commentary)

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + L-methionine + tRNAMet
-
 Trypanosoma brucei AMP + diphosphate + L-methionyl-tRNAMet
-
 ?
ATP + L-methionine + tRNAMet
-
 Trypanosoma brucei 927 AMP + diphosphate + L-methionyl-tRNAMet
-
 ?

Synonyms

Synonyms Comment Organism
methionyl-tRNA synthetase
-
 Trypanosoma brucei
MetRS
-
 Trypanosoma brucei

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Trypanosoma brucei

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
0.000028
-
 pH and temperature not specified in the publication Trypanosoma brucei N-(3-[[(3,5-dichlorophenyl)methyl]amino]propyl)-N'-thiophen-3-ylurea
0.000029
-
 pH and temperature not specified in the publication Trypanosoma brucei N-(3-[[(3,5-dichlorophenyl)methyl]amino]propyl)-N'-(3-hydroxyphenyl)urea
0.000039
-
 pH and temperature not specified in the publication Trypanosoma brucei N-(3-[[(3,5-dichlorophenyl)methyl]amino]propyl)-N'-(2-hydroxyphenyl)urea
0.000045
-
 pH and temperature not specified in the publication Trypanosoma brucei N-(3-[[(3-chloro-5-methoxyphenyl)methyl]amino]propyl)-N'-phenylurea
0.000057
-
 pH and temperature not specified in the publication Trypanosoma brucei N-(3-[[(3,5-dichlorophenyl)methyl]amino]propyl)-N'-phenylurea
0.000096
-
 pH and temperature not specified in the publication Trypanosoma brucei N-(3-[[(3-cyanophenyl)methyl]amino]propyl)-N'-thiophen-3-ylurea
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
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
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
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
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
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
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