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Literature summary for 1.4.1.3 extracted from

  • Zaganas, I.; Spanaki, C.; Karpusas, M.; Plaitakis, A.
    Substitution of Ser for Arg-443 in the regulatory domain of human housekeeping (GLUD1) glutamate dehydrogenase virtually abolishes basal activity and markedly alters the activation of the enzyme by ADP and L-leucine (2002), J. Biol. Chem., 277, 46552-46558.
    View publication on PubMed
Search for more literature for 1.4.1.3

Activating Compound

Activating Compound Comment Organism Structure
ADP activates Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
wild-type and mutant enzyme, expression in Sf21 cells using a baculovirus expression system Homo sapiens

Protein Variants

Protein Variants Comment Organism
M370L mutation does not abolish basal activity and does not abrogate the activation of the enzyme by L-Leu Homo sapiens
M415L mutation does not abolish basal activity and does not abrogate the activation of the enzyme by L-Leu Homo sapiens
R443S mutation abolishes basal activity and totally abrogates the activation of the enzyme by L-Leu, 1-10 mM, in absence of other effectors. When ADP, 0.025-0.1 mM, is present, L-Leu (0.3-6.0 mM) activates the mutant enzyme up to 2000%. The mutant enzyme is much less sensitive to ADP than the wild-type enzyme, however at 1 mM ADP the Vmax is comparable with that of wild-type enzyme GLUD1 GDH. KM-value for 2-oxoglutarate is similar to wild-type value Homo sapiens
S331T mutation does not abolish basal activity and does not abrogate the activation of the enzyme by L-Leu Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
GTP IC50 for wild-type GLUD1: 0.0122 mM, IC50 for mutant enzyme R443S: 0.0162 mM, IC50 for mutant enzyme M415L: 0.0147 mM, IC50 for mutant enzyme M370L: 0.0113 mM, IC50 for mutant enzyme S331T: 0.0108 mM Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
 additional information Km-values for 2-oxoglutaratefor mutant enzyme R443S, recombinant wild-type enzyme and wild-type enzyme from human liver Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-oxoglutarate + NADPH + NH3
-
 Homo sapiens L-glutamate + NADP+ + H2O
-
 ?

Synonyms

Synonyms Comment Organism
GLUD1
-
 Homo sapiens
housekeeping glutamate dehydrogenase
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0108
-
 IC50 for mutant enzyme S331T: 0.0108 mM Homo sapiens GTP
0.0113
-
 IC50 for mutant enzyme M370L: 0.0113 mM Homo sapiens GTP
0.0122
-
 IC50 for wild-type GLUD1: 0.0122 mM Homo sapiens GTP
0.0147
-
 IC50 for mutant enzyme M415L: 0.0147 mM Homo sapiens GTP
0.0162
-
 IC50 for mutant enzyme R443S: 0.0162 mM Homo sapiens GTP