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Literature summary for 6.1.1.17 extracted from

  • Balg, C.; Blais, S.P.; Bernier, S.; Huot, J.L.; Couture, M.; Lapointe, J.; Chenevert, R.
    Synthesis of beta-ketophosphonate analogs of glutamyl and glutaminyl adenylate, and selective inhibition of the corresponding bacterial aminoacyl-tRNA synthetases (2007), Bioorg. Med. Chem., 15, 295-304.
    View publication on PubMed

Application

Application Comment Organism
drug development design of better inhibitors specific for bacterial GluRSs, which are promising targets for antimicrobial therapy Escherichia coli

Inhibitors

Inhibitors Comment Organism Structure
Glu-AMS
-
Escherichia coli
glutaminyl-beta-ketophosphonate-adenosine i.e. Gln-KPA, competitive inhibition, non-cognate, binds at one site on the monomeric enzyme Escherichia coli
glutamyl-beta-ketophosphonate-adenosine i.e. Glu-KPA, selective, competitive inhibition of GluRS, binds at one site on the monomeric enzyme Escherichia coli

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Escherichia coli

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
55000
-
1 * 55000, recombinant His6-tagged GluRS, SDS-PAGE Escherichia coli

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + L-glutamate + tRNAGlu Escherichia coli
-
AMP + diphosphate + L-glutamyl-tRNAGlu
-
r

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + L-glutamate + tRNAGlu
-
Escherichia coli AMP + diphosphate + L-glutamyl-tRNAGlu
-
r
ATP + L-glutamate + tRNAGlu a two-step reaction Escherichia coli AMP + diphosphate + L-glutamyl-tRNAGlu
-
r

Subunits

Subunits Comment Organism
monomer 1 * 55000, recombinant His6-tagged GluRS, SDS-PAGE Escherichia coli

Synonyms

Synonyms Comment Organism
GluRS
-
Escherichia coli
Glutamyl-tRNA synthetase
-
Escherichia coli

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Escherichia coli

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.2
-
assay at Escherichia coli

Cofactor

Cofactor Comment Organism Structure
ATP
-
Escherichia coli

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information inhibition kinetics Escherichia coli
0.0000028
-
Glu-AMS pH 7.2, 37°C, versus L-glutamate Escherichia coli
0.018
-
glutamyl-beta-ketophosphonate-adenosine pH 7.2, 37°C, versus L-glutamate Escherichia coli
2.9
-
glutaminyl-beta-ketophosphonate-adenosine pH 7.2, 37°C, versus L-glutamate Escherichia coli