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Literature summary extracted from

  • Green, L.; Bullard, J.; Ribble, W.; Dean, F.; Ayers, D.; Ochsner, U.; Janjic, N.; Jarvis, T.
    Inhibition of methionyl-tRNA synthetase by REP8839 and effects of resistance mutations on enzyme activity (2009), Antimicrob. Agents Chemother., 53, 86-94.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
6.1.1.10 medicine REP8839 is a selective inhibitor of methionyl-tRNA synthetase with antibacterial activity against a variety of gram-positive organisms Staphylococcus aureus
6.1.1.10 medicine REP8839 is a selective inhibitor of methionyl-tRNA synthetase with antibacterial activity against a variety of gram-positive organisms Haemophilus influenzae
6.1.1.10 medicine REP8839 is a selective inhibitor of methionyl-tRNA synthetase with antibacterial activity against a variety of gram-positive organisms Escherichia coli
6.1.1.10 medicine REP8839 is a selective inhibitor of methionyl-tRNA synthetase with antibacterial activity against a variety of gram-positive organisms Homo sapiens
6.1.1.10 medicine REP8839 is a selective inhibitor of methionyl-tRNA synthetase with antibacterial activity against a variety of gram-positive organisms Streptococcus pneumoniae

Cloned(Commentary)

EC Number Cloned (Comment) Organism
6.1.1.10 bacterial strains, DH5alpha, containing pPROLar plasmids carrying the gene encoding MetRS1 are used Streptococcus pneumoniae
6.1.1.10 into an inducible Escherichia expression vector Staphylococcus aureus
6.1.1.10 plasmid pcDNA3.1MRS, containing a gene encoding hcMetRS, and plasmid pcDNA3.1MRSce2, containing a gene encoding full-length hmMetRS, are used, genes are inserted into pET100/D-TOPO vectors Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
6.1.1.10 A247E mutant MetRS Staphylococcus aureus
6.1.1.10 G223C mutant MetRS Staphylococcus aureus
6.1.1.10 G54A/A64P mutant MetRS Staphylococcus aureus
6.1.1.10 G54S mutant MetRS Staphylococcus aureus
6.1.1.10 I57N mutant MetRS Staphylococcus aureus
6.1.1.10 I57N/A247E mutant MetRS Staphylococcus aureus
6.1.1.10 I57N/G54S mutant MetRS Staphylococcus aureus
6.1.1.10 I57N/I238F mutant MetRS Staphylococcus aureus
6.1.1.10 I57N/V242F mutant MetRS Staphylococcus aureus
6.1.1.10 L213W mutant MetRS Staphylococcus aureus
6.1.1.10 V108M mutant MetRS Staphylococcus aureus

Inhibitors

EC Number Inhibitors Comment Organism Structure
6.1.1.10 REP8839
-
 Escherichia coli
6.1.1.10 REP8839
-
 Haemophilus influenzae
6.1.1.10 REP8839
-
 Homo sapiens
6.1.1.10 REP8839
-
 Staphylococcus aureus
6.1.1.10 REP8839
-
 Streptococcus pneumoniae

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
6.1.1.10 0.00027
-
 tRNAMet mutant G54S, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.00041
-
 tRNAMet mutant I57N/G54S, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.00045
-
 tRNAMet mutant I57N/A247E, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.00057
-
 tRNAMet mutant G54A/A64P, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.00089
-
 tRNAMet mutant I57N/I238F, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.00093
-
 tRNAMet mutant I57N, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.001
-
 tRNAMet wild-type, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.0013
-
 tRNAMet mutant A247E, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.0017
-
 tRNAMet mutant L213W, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.0025
-
 tRNAMet mutant G223C, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.0032
-
 tRNAMet mutant V108M, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.01
-
 tRNAMet mutant I57N/V242F, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.02
-
 L-methionine
-
 Homo sapiens
6.1.1.10 0.02
-
 L-methionine mutant I57N/V242F, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.025
-
 L-methionine mutant I57N, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.053
-
 L-methionine
-
 Streptococcus pneumoniae
6.1.1.10 0.075
-
 L-methionine mutant G54S, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.085
-
 ATP
-
 Homo sapiens
6.1.1.10 0.085
-
 L-methionine mutant I57N/I238F, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.1
-
 L-methionine mutant L213W, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.1
-
 L-methionine wild-type, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.14
-
 L-methionine mutant V108M, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.22
-
 L-methionine mutant A247E, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.25
-
 L-methionine
-
 Haemophilus influenzae
6.1.1.10 0.25
-
 L-methionine mutant I57N/A247E, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.36
-
 L-methionine mutant I57N/G54S, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.5
-
 ATP mutant G54S, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.5
-
 ATP wild-type, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.514
-
 ATP
-
 Streptococcus pneumoniae
6.1.1.10 0.595
-
 ATP mutant L213W, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.65
-
 ATP mutant V108M, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.68
-
 L-methionine mutant G223C, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.75
-
 ATP mutant G223C, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.76
-
 ATP mutant G54A/A64P, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.765
-
 ATP mutant I57N/G54S, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.81
-
 ATP mutant I57N/V242F, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 0.82
-
 ATP mutant I57N, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 1.07
-
 L-methionine mutant G54A/A64P, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 1.14
-
 ATP mutant A247E, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 1.2
-
 ATP
-
 Haemophilus influenzae
6.1.1.10 1.61
-
 ATP mutant I57N/I238F, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 2.23
-
 ATP mutant I57N/A247E, ATP:diphosphate exchange reaction Staphylococcus aureus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
6.1.1.10 cytoplasm hcMetRS Homo sapiens 5737
-
6.1.1.10 mitochondrion hmMetRS Homo sapiens 5739
-

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 Staphylococcus aureus
-
 AMP + diphosphate + L-methionyl-tRNAMet
-
 ?
6.1.1.10 ATP + L-methionine + tRNAMet Haemophilus influenzae
-
 AMP + diphosphate + L-methionyl-tRNAMet
-
 ?
6.1.1.10 ATP + L-methionine + tRNAMet Escherichia coli
-
 AMP + diphosphate + L-methionyl-tRNAMet
-
 ?
6.1.1.10 ATP + L-methionine + tRNAMet Homo sapiens
-
 AMP + diphosphate + L-methionyl-tRNAMet
-
 ?
6.1.1.10 ATP + L-methionine + tRNAMet Streptococcus pneumoniae
-
 AMP + diphosphate + L-methionyl-tRNAMet
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
6.1.1.10 Escherichia coli
-
-
-
6.1.1.10 Haemophilus influenzae
-
-
-
6.1.1.10 Homo sapiens
-
-
-
6.1.1.10 Staphylococcus aureus
-
-
-
6.1.1.10 Streptococcus pneumoniae
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
6.1.1.10 by ammonium sulfate precipitation and anion-exchange chromatography on a Source 15Q column Staphylococcus aureus
6.1.1.10 by ammonium sulfate precipitation and anion-exchange chromatography on a Source 15Q column Streptococcus pneumoniae
6.1.1.10 using Ni-nitrilotriacetic acid resin Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
6.1.1.10 ATP + L-methionine + tRNAMet
-
 Staphylococcus aureus AMP + diphosphate + L-methionyl-tRNAMet
-
 ?
6.1.1.10 ATP + L-methionine + tRNAMet
-
 Haemophilus influenzae AMP + diphosphate + L-methionyl-tRNAMet
-
 ?
6.1.1.10 ATP + L-methionine + tRNAMet
-
 Escherichia coli AMP + diphosphate + L-methionyl-tRNAMet
-
 ?
6.1.1.10 ATP + L-methionine + tRNAMet
-
 Homo sapiens AMP + diphosphate + L-methionyl-tRNAMet
-
 ?
6.1.1.10 ATP + L-methionine + tRNAMet
-
 Streptococcus pneumoniae AMP + diphosphate + L-methionyl-tRNAMet
-
 ?

Synonyms

EC Number Synonyms Comment Organism
6.1.1.10 hcMetRS
-
 Homo sapiens
6.1.1.10 hmMetRS
-
 Homo sapiens
6.1.1.10 methionyl-tRNA synthetase
-
 Staphylococcus aureus
6.1.1.10 methionyl-tRNA synthetase
-
 Haemophilus influenzae
6.1.1.10 methionyl-tRNA synthetase
-
 Escherichia coli
6.1.1.10 methionyl-tRNA synthetase
-
 Homo sapiens
6.1.1.10 methionyl-tRNA synthetase1
-
 Streptococcus pneumoniae
6.1.1.10 MetRS
-
 Staphylococcus aureus
6.1.1.10 MetRS
-
 Haemophilus influenzae
6.1.1.10 MetRS
-
 Escherichia coli
6.1.1.10 MetRS
-
 Homo sapiens
6.1.1.10 MetRS1
-
 Streptococcus pneumoniae

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
6.1.1.10 22
-
 tRNA aminoacylation assay at room temperature for 30 min for IC50 determinations Staphylococcus aureus
6.1.1.10 22
-
 tRNA aminoacylation assay at room temperature for 30 min for IC50 determinations Haemophilus influenzae
6.1.1.10 22
-
 tRNA aminoacylation assay at room temperature for 30 min for IC50 determinations Escherichia coli
6.1.1.10 22
-
 tRNA aminoacylation assay at room temperature for 30 min for IC50 determinations Homo sapiens
6.1.1.10 22
-
 tRNA aminoacylation assay at room temperature for 30 min for IC50 determinations Streptococcus pneumoniae
6.1.1.10 30
-
 tRNA aminoacylation assay at 30°C for 1 to 7.5 min for initial rate determination Staphylococcus aureus
6.1.1.10 30
-
 tRNA aminoacylation assay at 30°C for 1 to 7.5 min for initial rate determination Haemophilus influenzae
6.1.1.10 30
-
 tRNA aminoacylation assay at 30°C for 1 to 7.5 min for initial rate determination Escherichia coli
6.1.1.10 30
-
 tRNA aminoacylation assay at 30°C for 1 to 7.5 min for initial rate determination Homo sapiens
6.1.1.10 30
-
 tRNA aminoacylation assay at 30°C for 1 to 7.5 min for initial rate determination Streptococcus pneumoniae

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
6.1.1.10 0.001
-
 tRNAMet mutant G54A/A64P, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.002
-
 tRNAMet mutant I57N/G54S, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.008
-
 tRNAMet mutant I57N/A247E, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.009
-
 tRNAMet mutant G54S, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.023
-
 tRNAMet mutant I57N, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.037
-
 tRNAMet mutant G223C, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.057
-
 tRNAMet mutant A247E, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.066
-
 tRNAMet mutant I57N/I238F, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.124
-
 tRNAMet mutant I57N/V242F, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.49
-
 tRNAMet wild-type, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.54
-
 tRNAMet mutant L213W, aminoacylation reaction Staphylococcus aureus
6.1.1.10 0.74
-
 tRNAMet mutant V108M, aminoacylation reaction Staphylococcus aureus
6.1.1.10 1
-
 L-methionine mutant G54A/A64P, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 5
-
 L-methionine mutant G54S, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 6
-
 L-methionine mutant I57N/G54S, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 10
-
 L-methionine mutant G223C, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 10
-
 L-methionine mutant L213W, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 11
-
 L-methionine mutant A247E, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 11
-
 L-methionine mutant I57N/A247E, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 13
-
 L-methionine mutant I57N/I238F, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 14
-
 L-methionine mutant I57N, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 14
-
 L-methionine mutant I57N/V242F, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 15
-
 L-methionine mutant V108M, ATP:diphosphate exchange reaction Staphylococcus aureus
6.1.1.10 25
-
 L-methionine wild-type, ATP:diphosphate exchange reaction Staphylococcus aureus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
6.1.1.10 7.8
-
 tRNA aminoacylation assay Homo sapiens
6.1.1.10 8
-
 tRNA aminoacylation assay Staphylococcus aureus
6.1.1.10 8
-
 tRNA aminoacylation assay Haemophilus influenzae
6.1.1.10 8
-
 tRNA aminoacylation assay Escherichia coli
6.1.1.10 8
-
 tRNA aminoacylation assay Streptococcus pneumoniae

Cofactor

EC Number Cofactor Comment Organism Structure
6.1.1.10 ATP
-
 Staphylococcus aureus
6.1.1.10 ATP
-
 Haemophilus influenzae
6.1.1.10 ATP
-
 Escherichia coli
6.1.1.10 ATP
-
 Homo sapiens
6.1.1.10 ATP
-
 Streptococcus pneumoniae

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
6.1.1.10 0.00000001
-
 REP8839 wild-type Staphylococcus aureus
6.1.1.10 0.00000004
-
 REP8839 mutant L213W Staphylococcus aureus
6.1.1.10 0.000000055
-
 REP8839
-
 Streptococcus pneumoniae
6.1.1.10 0.00000006
-
 REP8839 mutant A247E Staphylococcus aureus
6.1.1.10 0.00000008
-
 REP8839 mutant I57N Staphylococcus aureus
6.1.1.10 0.00000011
-
 REP8839 mutant V108M Staphylococcus aureus
6.1.1.10 0.00000051
-
 REP8839 mutant G223C Staphylococcus aureus
6.1.1.10 0.00001
-
 REP8839 hmMetRS Homo sapiens
6.1.1.10 0.000015
-
 REP8839 mutant I57N/V242F Staphylococcus aureus
6.1.1.10 0.000023
-
 REP8839
-
 Haemophilus influenzae
6.1.1.10 0.00006
-
 REP8839 mutant I57N/A247E Staphylococcus aureus
6.1.1.10 0.000085
-
 REP8839 mutant G54S Staphylococcus aureus
6.1.1.10 0.000225
-
 REP8839
-
 Escherichia coli
6.1.1.10 0.00035
-
 REP8839 mutant I57N/I238F Staphylococcus aureus
6.1.1.10 0.0009
-
 REP8839 mutant I57N/G54S Staphylococcus aureus
6.1.1.10 0.0019
-
 REP8839 mutant G54A/A64P Staphylococcus aureus
6.1.1.10 0.02
-
 REP8839 hcMetRS, larger than 0.020 Homo sapiens