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Literature summary extracted from

  • Nordqvist, A.; Nilsson, M.T.; Roettger, S.; Odell, L.R.; Krajewski, W.W.; Evalena Andersson, C.; Larhed, M.; Mowbray, S.L.; Karlen, A.
    Evaluation of the amino acid binding site of Mycobacterium tuberculosis glutamine synthetase for drug discovery (2008), Bioorg. Med. Chem., 16, 5501-5513.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
6.3.1.2 (R)-2-[3-(diethoxyphosphoryl)phenylamino]-3-hydroxypropionic acid
-
Mycobacterium tuberculosis
6.3.1.2 (S)-2-[3-(diethoxyphosphoryl)phenylamino]-3-hydroxypropionic acid
-
Mycobacterium tuberculosis
6.3.1.2 (S)-3-hydroxy-2-(3-methylsulfanylphenylamino)propionic acid
-
Mycobacterium tuberculosis
6.3.1.2 (S)-3-hydroxy-2-(3-sulfamoylphenylamino)propionic acid
-
Mycobacterium tuberculosis
6.3.1.2 3-((R)-1-carboxy-2-hydroxyethylamino)benzoic acid
-
Mycobacterium tuberculosis
6.3.1.2 3-((S)-1-carboxy-2-hydroxyethylamino)benzoic acid
-
Mycobacterium tuberculosis
6.3.1.2 3-(carboxymethylamino)benzoic acid
-
Mycobacterium tuberculosis

Application

EC Number Application Comment Organism
6.3.1.2 drug development the enzyme is a potential antimycobacterial drug target Mycobacterium tuberculosis

Inhibitors

EC Number Inhibitors Comment Organism Structure
6.3.1.2 (2S)-2-amino-4-(methylsulfonyl)butanoic acid
-
Mycobacterium tuberculosis
6.3.1.2 (2S,5R)-2,6-diamino-5-hydroxyhexanoic acid docks at the amino acid binding site of the enzyme, structure, overview Mycobacterium tuberculosis
6.3.1.2 (3-methanesulfinylphenylamino)acetic acid 30% inhibition at 1.0 mM Mycobacterium tuberculosis
6.3.1.2 (R)-3-hydroxy-2-(3-sulfamoylphenylamino)propionic acid 33% inhibition at 1.0 mM Mycobacterium tuberculosis
6.3.1.2 (S)-3-hydroxy-2-(3-methanesulfinylphenylamino)propionic acid 13% inhibition at 1.0 mM Mycobacterium tuberculosis
6.3.1.2 2-amino-4-(hydroxyamino)butanoic acid
-
Mycobacterium tuberculosis
6.3.1.2 2-oxo-2,3-dihydro-1H-benzimidazole-5-sulfonamide 24% inhibition at 1.0 mM Mycobacterium tuberculosis
6.3.1.2 3-[(1H-1,2,4-triazol-3-ylcarbonyl)amino]benzoic acid 26% inhibition at 1.0 mM Mycobacterium tuberculosis
6.3.1.2 L-methionine sulfoximine
-
Mycobacterium tuberculosis
6.3.1.2 L-methionine-(S)-sulfoximine docks at the amino acid binding site of the enzyme, structure, overview Mycobacterium tuberculosis
6.3.1.2 additional information no inhibition by L-homoserine, (R)-3-hydroxy-2-(3-methanesulfinylphenylamino)propionic acid, (R)-3-hydroxy-2-(3-methylsulfanylphenylamino)propionic acid, (3-sulfamoylphenylamino)acetic acid, (3-methylsulfanylphenylamino)acetic acid, 2-amino-3-(2-phosphonomethylphenyl)propanoic acid, 2-amino-3-(2-aminomethylphenyl)propanoic acid, and methyl 2-amino-3-(2-phosphonomethylphenyl)propanoate, inhibitor screening and docking studies, overview Mycobacterium tuberculosis
6.3.1.2 N-(4-hydroxy-3-sulfophenyl)glycine 48% inhibition at 1.0 mM Mycobacterium tuberculosis
6.3.1.2 Phosphinothricin
-
Mycobacterium tuberculosis
6.3.1.2 [3-(diethoxyphosphoryl)phenylamino]acetic acid 42% inhibition at 1.0 mM Mycobacterium tuberculosis

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
6.3.1.2 Mg2+
-
Mycobacterium tuberculosis

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
6.3.1.2 ATP + L-glutamate + NH3 Mycobacterium tuberculosis glnA1 is essential for Mycobacterium tuberculosis virulence ADP + phosphate + L-glutamine
-
?
6.3.1.2 ATP + L-glutamate + NH3 Mycobacterium tuberculosis H37Rv glnA1 is essential for Mycobacterium tuberculosis virulence ADP + phosphate + L-glutamine
-
?

Organism

EC Number Organism UniProt Comment Textmining
6.3.1.2 Mycobacterium tuberculosis P9WN39 gene glnA1
-
6.3.1.2 Mycobacterium tuberculosis H37Rv P9WN39 gene glnA1
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
6.3.1.2 ATP + L-glutamate + NH3 glnA1 is essential for Mycobacterium tuberculosis virulence Mycobacterium tuberculosis ADP + phosphate + L-glutamine
-
?
6.3.1.2 ATP + L-glutamate + NH3 amino acid binding site and structure, overview Mycobacterium tuberculosis ADP + phosphate + L-glutamine
-
?
6.3.1.2 ATP + L-glutamate + NH3 glnA1 is essential for Mycobacterium tuberculosis virulence Mycobacterium tuberculosis H37Rv ADP + phosphate + L-glutamine
-
?
6.3.1.2 ATP + L-glutamate + NH3 amino acid binding site and structure, overview Mycobacterium tuberculosis H37Rv ADP + phosphate + L-glutamine
-
?

Synonyms

EC Number Synonyms Comment Organism
6.3.1.2 Glutamine synthetase
-
Mycobacterium tuberculosis

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
6.3.1.2 22
-
assay at room temperature Mycobacterium tuberculosis

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
6.3.1.2 7.5
-
assay at Mycobacterium tuberculosis

Cofactor

EC Number Cofactor Comment Organism Structure
6.3.1.2 ATP
-
Mycobacterium tuberculosis

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
6.3.1.2 0.0019
-
pH 7.5, 22°C Mycobacterium tuberculosis Phosphinothricin
6.3.1.2 0.026
-
pH 7.5, 22°C Mycobacterium tuberculosis 2-amino-4-(hydroxyamino)butanoic acid
6.3.1.2 0.033
-
pH 7.5, 22°C Mycobacterium tuberculosis (2S)-2-amino-4-(methylsulfonyl)butanoic acid
6.3.1.2 0.051
-
pH 7.5, 22°C Mycobacterium tuberculosis L-methionine-(S)-sulfoximine
6.3.1.2 0.056 0.058 dependent on the solvent, pH 7.5, 22°C Mycobacterium tuberculosis (2S,5R)-2,6-diamino-5-hydroxyhexanoic acid
6.3.1.2 0.076
-
pH 7.5, 22°C Mycobacterium tuberculosis Phosphinothricin
6.3.1.2 0.081
-
pH 7.5, 22°C Mycobacterium tuberculosis L-methionine sulfoximine