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Literature summary for 3.5.1.2 extracted from

  • Thangavelu, K.; Chong, Q.Y.; Low, B.C.; Sivaraman, J.
    Structural basis for the active site inhibition mechanism of human kidney-type glutaminase (KGA) (2014), Sci. Rep., 4, 3827.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.5.1.2

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21 (DE3)-RIL-Codon plus cells Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
catalytic domain of isoform KGA in complex with 6-diazo-5-oxo-L-norleucine, hanging drop vapor diffusion method, using 0.1 M Bis-Tris propane (pH 7.2) and 1.8 M LiSO4 Homo sapiens

Protein Variants

Protein Variants Comment Organism
K289A the mutant shows about 10% activity compared to the wild type enzyme Homo sapiens
S286A the mutant shows about 10% activity compared to the wild type enzyme Homo sapiens
Y249A the mutant shows about 10% activity compared to the wild type enzyme Homo sapiens
Y466A the mutant shows about 18% activity compared to the wild type enzyme Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
6-diazo-5-oxo-L-norleucine active site inhibitor, about 53% inhibition at about 1 mM Homo sapiens
azaserine about 19% inhibition at about 1 mM Homo sapiens
glufosinate ammonium about 23% inhibition at about 1 mM Homo sapiens
L-methionine sulfoximine about 21% inhibition at about 1 mM Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
L-glutamine + H2O Homo sapiens
-
 L-glutamate + NH3
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens O94925
-
-

Purification (Commentary)

Purification (Comment) Organism
Ni-NTA column chromatpgraphy and gel filtration Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
kidney
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
6-diazo-5-oxo-L-norleucine + H2O the nucleophilic attack of Ser286 sidechain on 6-diazo-5-oxo-L-norleucine releases the diazo group (N2) from the inhibitor and results in the formation of an enzyme-inhibitor complex Homo sapiens ?
-
 ?
L-glutamine + H2O
-
 Homo sapiens L-glutamate + NH3
-
 ?

Synonyms

Synonyms Comment Organism
GLS1
-
 Homo sapiens
KGA isoform Homo sapiens
kidney-type glutaminase
-
 Homo sapiens