Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.5.1.2 extracted from

  • Thomas, A.G.; Rojas, C.; Tanega, C.; Shen, M.; Simeonov, A.; Boxer, M.B.; Auld, D.S.; Ferraris, D.V.; Tsukamoto, T.; Slusher, B.S.
    Kinetic characterization of ebselen, chelerythrine and apomorphine as glutaminase inhibitors (2013), Biochem. Biophys. Res. Commun., 438, 243-248.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
2-phenyl isoindolin-1-one
-
Mus musculus
2-phenylbenzo[d] isoxazol-3(2H)-one
-
Mus musculus
2-phenylbenzo[d]isothiazol-3(2H)-one
-
Mus musculus
6-diazo-5-oxo-Lnorleucine time-dependent inhibition Mus musculus
apomorphine competitive inhibition, i.e. 5,6,6a,7-tetrahydro-6-methyl-4H-dibenzo[de,g]quinoline-10,11-diol Mus musculus
Berberine
-
Mus musculus
bis-2-(5-phenylacetimido-1,2,4-thiadiazol-2-yl)ethyl sulfide uncompetitive inhibition Mus musculus
chelerythrine competitive inhibition, i.e. 1,2-dimethoxy-N-methyl[1,3]benzodioxolo[5,6-c]phenanthridinium Mus musculus
ebselen mixed non-competitive inhibition, i.e. 2-phenyl-1,2-benzisoselenazol-3[2H]-one Mus musculus
nitidine
-
Mus musculus
norsanguinarine
-
Mus musculus
R(-)-apocodeine
-
Mus musculus
R(-)-propylnorapomorphine
-
Mus musculus
sanguinarine
-
Mus musculus

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Mus musculus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-glutamine + H2O
-
Mus musculus L-glutamate + NH3
-
?

Synonyms

Synonyms Comment Organism
GAC c-type glutaminase Mus musculus
GLA liver glutaminase Mus musculus
GLS
-
Mus musculus
KGA kidney-type glutaminase Mus musculus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000015
-
ebselen pH and temperature not specified in the publication Mus musculus
0.000125
-
bis-2-(5-phenylacetimido-1,2,4-thiadiazol-2-yl)ethyl sulfide pH and temperature not specified in the publication Mus musculus
0.00027
-
chelerythrine pH and temperature not specified in the publication Mus musculus
0.00232
-
apomorphine pH and temperature not specified in the publication Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000009
-
pH and temperature not specified in the publication Mus musculus ebselen
0.00003
-
pH and temperature not specified in the publication Mus musculus chelerythrine
0.0001
-
pH and temperature not specified in the publication Mus musculus sanguinarine
0.0006
-
pH and temperature not specified in the publication Mus musculus apomorphine
0.0009
-
pH and temperature not specified in the publication Mus musculus R(-)-propylnorapomorphine
0.004
-
pH and temperature not specified in the publication Mus musculus R(-)-apocodeine
0.009
-
pH and temperature not specified in the publication Mus musculus nitidine
0.02
-
pH and temperature not specified in the publication Mus musculus 2-phenylbenzo[d] isoxazol-3(2H)-one
0.1
-
IC50 above 0.1 mM, pH and temperature not specified in the publication Mus musculus Berberine
0.1
-
IC50 above 0.1 mM, pH and temperature not specified in the publication Mus musculus 2-phenyl isoindolin-1-one
0.1
-
IC50 above 0.1 mM, pH and temperature not specified in the publication Mus musculus norsanguinarine