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Literature summary for 6.3.1.2 extracted from

  • Nilsson, M.T.; Krajewski, W.W.; Yellagunda, S.; Prabhumurthy, S.; Chamarahally, G.N.; Siddamadappa, C.; Srinivasa, B.R.; Yahiaoui, S.; Larhed, M.; Karlen, A.; Jones, T.A.; Mowbray, S.L.
    Structural basis for the inhibition of Mycobacterium tuberculosis glutamine synthetase by novel ATP-competitive inhibitors (2009), J. Mol. Biol., 393, 504-513.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
complex of the enzyme with the purine analogue 1-[(3,4-dichlorophenyl)methyl]-3,7-dimethyl-8-morpholin-4-yl-purine-2,6-dione alone to 2.55 A resolution, and in complex with 1-[(3,4-dichlorophenyl)methyl]-3,7-dimethyl-8-morpholin-4-yl-purine-2,6-dione together with methionine sulfoximine phosphate, magnesium and phosphate, to 2.2 A resolution. The former represents a relaxed, inactive conformation of the enzyme, while the latter is a taut, active one. Compound 1-[(3,4-dichlorophenyl)methyl]-3,7-dimethyl-8-morpholin-4-yl-purine-2,6-dione binds at the same position in the nucleotide site, regardless of the conformational state Mycobacterium tuberculosis

Inhibitors

Inhibitors Comment Organism Structure
1-[(3,4-dichlorophenyl)methyl]-3,7-dimethyl-8-morpholin-4-yl-purine-2,6-dione
-
Mycobacterium tuberculosis
DMSO about 15% activation at 2% Mycobacterium tuberculosis
Mg2+ activiation up to 25 mM, inhibition above Mycobacterium tuberculosis

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.5
-
ATP pH 7.5 Mycobacterium tuberculosis
10.8
-
NH4+ pH 7.5 Mycobacterium tuberculosis
21.6
-
glutamate pH 7.5 Mycobacterium tuberculosis

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ activation up to 25 mM, inhibition above Mycobacterium tuberculosis

Organism

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + glutamate + NH4+
-
Mycobacterium tuberculosis ADP + phosphate + L-glutamine
-
?
ATP + glutamate + NH4+
-
Mycobacterium tuberculosis H37Rv ADP + phosphate + L-glutamine
-
?

pH Optimum

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0025
-
-
Mycobacterium tuberculosis 1-[(3,4-dichlorophenyl)methyl]-3,7-dimethyl-8-morpholin-4-yl-purine-2,6-dione