Literature summary for 6.3.1.2 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.

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Activating Compound

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

Application

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

Inhibitors

Inhibitors	Comment	Organism	Structure
(2S)-2-amino-4-(methylsulfonyl)butanoic acid	-	Mycobacterium tuberculosis
(2S,5R)-2,6-diamino-5-hydroxyhexanoic acid	docks at the amino acid binding site of the enzyme, structure, overview	Mycobacterium tuberculosis
(3-methanesulfinylphenylamino)acetic acid	30% inhibition at 1.0 mM	Mycobacterium tuberculosis
(R)-3-hydroxy-2-(3-sulfamoylphenylamino)propionic acid	33% inhibition at 1.0 mM	Mycobacterium tuberculosis
(S)-3-hydroxy-2-(3-methanesulfinylphenylamino)propionic acid	13% inhibition at 1.0 mM	Mycobacterium tuberculosis
2-amino-4-(hydroxyamino)butanoic acid	-	Mycobacterium tuberculosis
2-oxo-2,3-dihydro-1H-benzimidazole-5-sulfonamide	24% inhibition at 1.0 mM	Mycobacterium tuberculosis
3-[(1H-1,2,4-triazol-3-ylcarbonyl)amino]benzoic acid	26% inhibition at 1.0 mM	Mycobacterium tuberculosis
L-methionine sulfoximine	-	Mycobacterium tuberculosis
L-methionine-(S)-sulfoximine	docks at the amino acid binding site of the enzyme, structure, overview	Mycobacterium tuberculosis
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
N-(4-hydroxy-3-sulfophenyl)glycine	48% inhibition at 1.0 mM	Mycobacterium tuberculosis
Phosphinothricin	-	Mycobacterium tuberculosis
[3-(diethoxyphosphoryl)phenylamino]acetic acid	42% inhibition at 1.0 mM	Mycobacterium tuberculosis

Metals/Ions

Metals/Ions	Comment	Organism	Structure
Mg2+	-	Mycobacterium tuberculosis

Natural Substrates/ Products (Substrates)

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

Organism

Organism	UniProt	Comment	Textmining
Mycobacterium tuberculosis	P9WN39	gene glnA1	-
Mycobacterium tuberculosis H37Rv	P9WN39	gene glnA1	-

Substrates and Products (Substrate)

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

Synonyms

Synonyms	Comment	Organism
Glutamine synthetase	-	Mycobacterium tuberculosis

Temperature Optimum [°C]

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

pH Optimum

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

Cofactor

Cofactor	Comment	Organism	Structure
ATP	-	Mycobacterium tuberculosis

IC50 Value

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

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Release 2023.1 (January 2023)