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Literature summary for 6.1.1.10 extracted from
- Inhibition of methionyl-tRNA synthetase by REP8839 and effects of resistance mutations on enzyme activity (2009), Antimicrob. Agents Chemother., 53, 86-94.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | REP8839 is a selective inhibitor of methionyl-tRNA synthetase with antibacterial activity against a variety of gram-positive organisms | Staphylococcus aureus |
| medicine | REP8839 is a selective inhibitor of methionyl-tRNA synthetase with antibacterial activity against a variety of gram-positive organisms | Haemophilus influenzae |
| medicine | REP8839 is a selective inhibitor of methionyl-tRNA synthetase with antibacterial activity against a variety of gram-positive organisms | Escherichia coli |
| medicine | REP8839 is a selective inhibitor of methionyl-tRNA synthetase with antibacterial activity against a variety of gram-positive organisms | Homo sapiens |
| medicine | REP8839 is a selective inhibitor of methionyl-tRNA synthetase with antibacterial activity against a variety of gram-positive organisms | Streptococcus pneumoniae |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| bacterial strains, DH5alpha, containing pPROLar plasmids carrying the gene encoding MetRS1 are used | Streptococcus pneumoniae |
| into an inducible Escherichia expression vector | Staphylococcus aureus |
| 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
| Protein Variants | Comment | Organism |
|---|---|---|
| A247E | mutant MetRS | Staphylococcus aureus |
| G223C | mutant MetRS | Staphylococcus aureus |
| G54A/A64P | mutant MetRS | Staphylococcus aureus |
| G54S | mutant MetRS | Staphylococcus aureus |
| I57N | mutant MetRS | Staphylococcus aureus |
| I57N/A247E | mutant MetRS | Staphylococcus aureus |
| I57N/G54S | mutant MetRS | Staphylococcus aureus |
| I57N/I238F | mutant MetRS | Staphylococcus aureus |
| I57N/V242F | mutant MetRS | Staphylococcus aureus |
| L213W | mutant MetRS | Staphylococcus aureus |
| V108M | mutant MetRS | Staphylococcus aureus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| REP8839 | - |
Escherichia coli |  |
| REP8839 | - |
Haemophilus influenzae | |
| REP8839 | - |
Homo sapiens | |
| REP8839 | - |
Staphylococcus aureus | |
| REP8839 | - |
Streptococcus pneumoniae | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00027 | - |
tRNAMet | mutant G54S, aminoacylation reaction | Staphylococcus aureus | |
| 0.00041 | - |
tRNAMet | mutant I57N/G54S, aminoacylation reaction | Staphylococcus aureus | |
| 0.00045 | - |
tRNAMet | mutant I57N/A247E, aminoacylation reaction | Staphylococcus aureus | |
| 0.00057 | - |
tRNAMet | mutant G54A/A64P, aminoacylation reaction | Staphylococcus aureus | |
| 0.00089 | - |
tRNAMet | mutant I57N/I238F, aminoacylation reaction | Staphylococcus aureus | |
| 0.00093 | - |
tRNAMet | mutant I57N, aminoacylation reaction | Staphylococcus aureus | |
| 0.001 | - |
tRNAMet | wild-type, aminoacylation reaction | Staphylococcus aureus | |
| 0.0013 | - |
tRNAMet | mutant A247E, aminoacylation reaction | Staphylococcus aureus | |
| 0.0017 | - |
tRNAMet | mutant L213W, aminoacylation reaction | Staphylococcus aureus | |
| 0.0025 | - |
tRNAMet | mutant G223C, aminoacylation reaction | Staphylococcus aureus | |
| 0.0032 | - |
tRNAMet | mutant V108M, aminoacylation reaction | Staphylococcus aureus | |
| 0.01 | - |
tRNAMet | mutant I57N/V242F, aminoacylation reaction | Staphylococcus aureus | |
| 0.02 | - |
L-methionine | - |
Homo sapiens | |
| 0.02 | - |
L-methionine | mutant I57N/V242F, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.025 | - |
L-methionine | mutant I57N, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.053 | - |
L-methionine | - |
Streptococcus pneumoniae | |
| 0.075 | - |
L-methionine | mutant G54S, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.085 | - |
ATP | - |
Homo sapiens | |
| 0.085 | - |
L-methionine | mutant I57N/I238F, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.1 | - |
L-methionine | mutant L213W, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.1 | - |
L-methionine | wild-type, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.14 | - |
L-methionine | mutant V108M, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.22 | - |
L-methionine | mutant A247E, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.25 | - |
L-methionine | - |
Haemophilus influenzae | |
| 0.25 | - |
L-methionine | mutant I57N/A247E, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.36 | - |
L-methionine | mutant I57N/G54S, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.5 | - |
ATP | mutant G54S, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.5 | - |
ATP | wild-type, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.514 | - |
ATP | - |
Streptococcus pneumoniae | |
| 0.595 | - |
ATP | mutant L213W, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.65 | - |
ATP | mutant V108M, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.68 | - |
L-methionine | mutant G223C, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.75 | - |
ATP | mutant G223C, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.76 | - |
ATP | mutant G54A/A64P, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.765 | - |
ATP | mutant I57N/G54S, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.81 | - |
ATP | mutant I57N/V242F, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 0.82 | - |
ATP | mutant I57N, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 1.07 | - |
L-methionine | mutant G54A/A64P, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 1.14 | - |
ATP | mutant A247E, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 1.2 | - |
ATP | - |
Haemophilus influenzae | |
| 1.61 | - |
ATP | mutant I57N/I238F, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 2.23 | - |
ATP | mutant I57N/A247E, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| cytoplasm | hcMetRS | Homo sapiens | 5737 | - |
| mitochondrion | hmMetRS | Homo sapiens | 5739 | - |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + L-methionine + tRNAMet | Staphylococcus aureus | - |
AMP + diphosphate + L-methionyl-tRNAMet | - |
? | |
| ATP + L-methionine + tRNAMet | Haemophilus influenzae | - |
AMP + diphosphate + L-methionyl-tRNAMet | - |
? | |
| ATP + L-methionine + tRNAMet | Escherichia coli | - |
AMP + diphosphate + L-methionyl-tRNAMet | - |
? | |
| ATP + L-methionine + tRNAMet | Homo sapiens | - |
AMP + diphosphate + L-methionyl-tRNAMet | - |
? | |
| ATP + L-methionine + tRNAMet | Streptococcus pneumoniae | - |
AMP + diphosphate + L-methionyl-tRNAMet | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Escherichia coli | - |
- |
- |
| Haemophilus influenzae | - |
- |
- |
| Homo sapiens | - |
- |
- |
| Staphylococcus aureus | - |
- |
- |
| Streptococcus pneumoniae | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| by ammonium sulfate precipitation and anion-exchange chromatography on a Source 15Q column | Staphylococcus aureus |
| by ammonium sulfate precipitation and anion-exchange chromatography on a Source 15Q column | Streptococcus pneumoniae |
| using Ni-nitrilotriacetic acid resin | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + L-methionine + tRNAMet | - |
Staphylococcus aureus | AMP + diphosphate + L-methionyl-tRNAMet | - |
? | |
| ATP + L-methionine + tRNAMet | - |
Haemophilus influenzae | AMP + diphosphate + L-methionyl-tRNAMet | - |
? | |
| ATP + L-methionine + tRNAMet | - |
Escherichia coli | AMP + diphosphate + L-methionyl-tRNAMet | - |
? | |
| ATP + L-methionine + tRNAMet | - |
Homo sapiens | AMP + diphosphate + L-methionyl-tRNAMet | - |
? | |
| ATP + L-methionine + tRNAMet | - |
Streptococcus pneumoniae | AMP + diphosphate + L-methionyl-tRNAMet | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| hcMetRS | - |
Homo sapiens |
| hmMetRS | - |
Homo sapiens |
| methionyl-tRNA synthetase | - |
Staphylococcus aureus |
| methionyl-tRNA synthetase | - |
Haemophilus influenzae |
| methionyl-tRNA synthetase | - |
Escherichia coli |
| methionyl-tRNA synthetase | - |
Homo sapiens |
| methionyl-tRNA synthetase1 | - |
Streptococcus pneumoniae |
| MetRS | - |
Staphylococcus aureus |
| MetRS | - |
Haemophilus influenzae |
| MetRS | - |
Escherichia coli |
| MetRS | - |
Homo sapiens |
| MetRS1 | - |
Streptococcus pneumoniae |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 22 | - |
tRNA aminoacylation assay at room temperature for 30 min for IC50 determinations | Staphylococcus aureus |
| 22 | - |
tRNA aminoacylation assay at room temperature for 30 min for IC50 determinations | Haemophilus influenzae |
| 22 | - |
tRNA aminoacylation assay at room temperature for 30 min for IC50 determinations | Escherichia coli |
| 22 | - |
tRNA aminoacylation assay at room temperature for 30 min for IC50 determinations | Homo sapiens |
| 22 | - |
tRNA aminoacylation assay at room temperature for 30 min for IC50 determinations | Streptococcus pneumoniae |
| 30 | - |
tRNA aminoacylation assay at 30°C for 1 to 7.5 min for initial rate determination | Staphylococcus aureus |
| 30 | - |
tRNA aminoacylation assay at 30°C for 1 to 7.5 min for initial rate determination | Haemophilus influenzae |
| 30 | - |
tRNA aminoacylation assay at 30°C for 1 to 7.5 min for initial rate determination | Escherichia coli |
| 30 | - |
tRNA aminoacylation assay at 30°C for 1 to 7.5 min for initial rate determination | Homo sapiens |
| 30 | - |
tRNA aminoacylation assay at 30°C for 1 to 7.5 min for initial rate determination | Streptococcus pneumoniae |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.001 | - |
tRNAMet | mutant G54A/A64P, aminoacylation reaction | Staphylococcus aureus | |
| 0.002 | - |
tRNAMet | mutant I57N/G54S, aminoacylation reaction | Staphylococcus aureus | |
| 0.008 | - |
tRNAMet | mutant I57N/A247E, aminoacylation reaction | Staphylococcus aureus | |
| 0.009 | - |
tRNAMet | mutant G54S, aminoacylation reaction | Staphylococcus aureus | |
| 0.023 | - |
tRNAMet | mutant I57N, aminoacylation reaction | Staphylococcus aureus | |
| 0.037 | - |
tRNAMet | mutant G223C, aminoacylation reaction | Staphylococcus aureus | |
| 0.057 | - |
tRNAMet | mutant A247E, aminoacylation reaction | Staphylococcus aureus | |
| 0.066 | - |
tRNAMet | mutant I57N/I238F, aminoacylation reaction | Staphylococcus aureus | |
| 0.124 | - |
tRNAMet | mutant I57N/V242F, aminoacylation reaction | Staphylococcus aureus | |
| 0.49 | - |
tRNAMet | wild-type, aminoacylation reaction | Staphylococcus aureus | |
| 0.54 | - |
tRNAMet | mutant L213W, aminoacylation reaction | Staphylococcus aureus | |
| 0.74 | - |
tRNAMet | mutant V108M, aminoacylation reaction | Staphylococcus aureus | |
| 1 | - |
L-methionine | mutant G54A/A64P, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 5 | - |
L-methionine | mutant G54S, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 6 | - |
L-methionine | mutant I57N/G54S, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 10 | - |
L-methionine | mutant G223C, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 10 | - |
L-methionine | mutant L213W, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 11 | - |
L-methionine | mutant A247E, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 11 | - |
L-methionine | mutant I57N/A247E, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 13 | - |
L-methionine | mutant I57N/I238F, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 14 | - |
L-methionine | mutant I57N, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 14 | - |
L-methionine | mutant I57N/V242F, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 15 | - |
L-methionine | mutant V108M, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
| 25 | - |
L-methionine | wild-type, ATP:diphosphate exchange reaction | Staphylococcus aureus | |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.8 | - |
tRNA aminoacylation assay | Homo sapiens |
| 8 | - |
tRNA aminoacylation assay | Staphylococcus aureus |
| 8 | - |
tRNA aminoacylation assay | Haemophilus influenzae |
| 8 | - |
tRNA aminoacylation assay | Escherichia coli |
| 8 | - |
tRNA aminoacylation assay | Streptococcus pneumoniae |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Staphylococcus aureus | |
| ATP | - |
Haemophilus influenzae | |
| ATP | - |
Escherichia coli | |
| ATP | - |
Homo sapiens | |
| ATP | - |
Streptococcus pneumoniae | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00000001 | - |
REP8839 | wild-type | Staphylococcus aureus | |
| 0.00000004 | - |
REP8839 | mutant L213W | Staphylococcus aureus | |
| 0.000000055 | - |
REP8839 | - |
Streptococcus pneumoniae | |
| 0.00000006 | - |
REP8839 | mutant A247E | Staphylococcus aureus | |
| 0.00000008 | - |
REP8839 | mutant I57N | Staphylococcus aureus | |
| 0.00000011 | - |
REP8839 | mutant V108M | Staphylococcus aureus | |
| 0.00000051 | - |
REP8839 | mutant G223C | Staphylococcus aureus | |
| 0.00001 | - |
REP8839 | hmMetRS | Homo sapiens | |
| 0.000015 | - |
REP8839 | mutant I57N/V242F | Staphylococcus aureus | |
| 0.000023 | - |
REP8839 | - |
Haemophilus influenzae | |
| 0.00006 | - |
REP8839 | mutant I57N/A247E | Staphylococcus aureus | |
| 0.000085 | - |
REP8839 | mutant G54S | Staphylococcus aureus | |
| 0.000225 | - |
REP8839 | - |
Escherichia coli | |
| 0.00035 | - |
REP8839 | mutant I57N/I238F | Staphylococcus aureus | |
| 0.0009 | - |
REP8839 | mutant I57N/G54S | Staphylococcus aureus | |
| 0.0019 | - |
REP8839 | mutant G54A/A64P | Staphylococcus aureus | |
| 0.02 | - |
REP8839 | hcMetRS, larger than 0.020 | Homo sapiens | |
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