Cloned (Comment) | Organism |
---|---|
expressed in Escherichia coli C41(DE3)pLysS cells | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
D520K | the mutant of isoform KGA is 0.14fold more sensitive against inhibitor AV-1 compared to the wild type enzyme | Homo sapiens |
F318Y/F322S | the mutant of isoform KGA is 1.1fold less sensitive against inhibitor AV-1 and more than 1250fold less sensitive against BPTES compared to the wild type enzyme | Homo sapiens |
H519Q | the mutant of isoform KGA is 0.79fold more sensitive against inhibitor AV-1 compared to the wild type enzyme | Homo sapiens |
H519Q/D520K | the mutant of isoform KGA is 0.11fold more sensitive against inhibitor AV-1 compared to the wild type enzyme | Homo sapiens |
K453D | the mutant of isoform GAB is 14.9fold less sensitive against inhibitor AV-1 compared to the wild type enzyme | Homo sapiens |
Q452H | the mutant of isoform GAB is 4.7fold less sensitive against inhibitor AV-1 compared to the wild type enzyme | Homo sapiens |
Q452H/K453D | the mutant of isoform GAB is 18.4fold less sensitive against inhibitor AV-1 compared to the wild type enzyme | Homo sapiens |
Y394L | the mutant of isoform KGA is 0.67fold more sensitive against inhibitor AV-1 and more than 1250fold less sensitive against BPTES compared to the wild type enzyme | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(2R)-1-(2-formyl-3,6-dihydroxy-5-methoxycyclohexa-1,4-dien-1-yl)tridecan-2-yl acetate | - |
Homo sapiens | |
(2R)-1-(2-hydroxy-5-methoxy-3,6-dioxocyclohexa-1,4-dien-1-yl)pentadecan-2-yl acetate | - |
Homo sapiens | |
(2R)-1-(2-hydroxy-5-methoxy-3,6-dioxocyclohexa-1,4-dien-1-yl)tridecan-2-yl acetate | - |
Homo sapiens | |
(2R)-1-(3,6-dihydroxy-5-methoxycyclohexa-1,4-dien-1-yl)tridecan-2-yl acetate | - |
Homo sapiens | |
(2R)-1-(5-methoxy-3,6-dioxocyclohexa-1,4-dien-1-yl)pentadecan-2-yl acetate | - |
Homo sapiens | |
(2R)-1-(5-methoxy-3,6-dioxocyclohexa-1,4-dien-1-yl)tridecan-2-yl acetate | - |
Homo sapiens | |
(2R)-1-[3-(acetyloxy)-6-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl]pentadecan-2-yl acetate | - |
Homo sapiens | |
(2R)-1-[3-(acetyloxy)-6-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl]tridecan-2-yl acetate | - |
Homo sapiens | |
(2S)-1-(5-methoxycyclohexa-1,4-dien-1-yl)heptan-2-ol | - |
Homo sapiens | |
2-hydroxy-5-methoxy-3-tridecylcyclohexa-2,5-diene-1,4-dione | - |
Homo sapiens | |
2-methoxy-6-pentadecylcyclohexa-2,5-diene-1,4-dione | - |
Homo sapiens | |
2-methoxy-6-tridecylcyclohexa-2,5-diene-1,4-dione | - |
Homo sapiens | |
2-methyl-5-[(7Z)-pentadec-7-en-1-yl]cyclohexa-1,4-diene-1,3-diol | - |
Homo sapiens | |
2-methyl-5-[(7Z)-tridec-7-en-1-yl]cyclohexa-1,4-diene-1,3-diol | - |
Homo sapiens | |
3-[(2S)-2-hydroxypentadecyl]-5-methoxycyclohexa-2,5-dien-1-ol | - |
Homo sapiens | |
4-hydroxy-2-methoxy-6-(2-oxopentadecyl)cyclohexa-2,5-dien-1-yl acetate | - |
Homo sapiens | |
5-[(6Z)-13-(3,5-dihydroxy-4-methylcyclohexa-1,4-dien-1-yl)tridec-6-en-1-yl]-2-methylbenzene-1,3-diol | - |
Homo sapiens | |
5-[(6Z)-13-(3,5-dihydroxy-4-methylcyclohexa-1,4-dien-1-yl)tridec-6-en-1-yl]benzene-1,3-diol | - |
Homo sapiens | |
5-[(6Z)-13-(3-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl)tridec-6-en-1-yl]benzene-1,3-diol | - |
Homo sapiens | |
5-[(7Z)-13-(3-hydroxy-5-methoxyphenyl)tridec-7-en-1-yl]-2-methylcyclohexa-1,4-diene-1,3-diol | - |
Homo sapiens | |
5-[(7Z)-15-(3-hydroxy-5-methoxyphenyl)pentadec-7-en-1-yl]-2-methylcyclohexa-1,4-diene-1,3-diol | - |
Homo sapiens | |
5-[(7Z)-pentadec-7-en-1-yl]cyclohexa-1,4-diene-1,3-diol | - |
Homo sapiens | |
5-[(7Z)-tridec-7-en-1-yl]cyclohexa-1,4-diene-1,3-diol | - |
Homo sapiens | |
5-[(8Z)-15-(3,5-dihydroxy-4-methylcyclohexa-1,4-dien-1-yl)pentadec-8-en-1-yl]-2-methylbenzene-1,3-diol | - |
Homo sapiens | |
5-[(8Z)-15-(3,5-dihydroxy-4-methylcyclohexa-1,4-dien-1-yl)pentadec-8-en-1-yl]benzene-1,3-diol | - |
Homo sapiens | |
5-[(8Z)-15-(3-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl)pentadec-8-en-1-yl]benzene-1,3-diol | - |
Homo sapiens | |
5-[14-(3-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl)tetradecyl]benzene-1,3-diol | - |
Homo sapiens | |
6-diazo-5-oxo-L-norleucine | - |
Homo sapiens | |
bis-2-(5-phenylacetimido-1,2,4-thiadiazol-2-yl) ethyl sulfide | glutaminase-1-selective inhibitor | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
L-glutamine + H2O | Homo sapiens | - |
L-glutamate + NH3 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Purification (Comment) | Organism |
---|---|
Ni+-charged affinity column chromatography | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
A-549 cell | - |
Homo sapiens | - |
Detroit-551 cell | - |
Homo sapiens | - |
Hep-G2 cell | - |
Homo sapiens | - |
MCF-7 cell | - |
Homo sapiens | - |
NCI-H460 cell | - |
Homo sapiens | - |
SF-268 cell | - |
Homo sapiens | - |
WI-38 cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
L-glutamine + H2O | - |
Homo sapiens | L-glutamate + NH3 | - |
? |
Synonyms | Comment | Organism |
---|---|---|
GAB | GLS2-isoform | Homo sapiens |
GAC | GLS1-isoform | Homo sapiens |
GLS1 | - |
Homo sapiens |
GLS2 | - |
Homo sapiens |
glutaminase-1 | - |
Homo sapiens |
glutaminase-2 | - |
Homo sapiens |
glutaminase-B | - |
Homo sapiens |
KGA | GLS1-isoform | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00008 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | bis-2-(5-phenylacetimido-1,2,4-thiadiazol-2-yl) ethyl sulfide | |
0.00026 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | (2R)-1-(3,6-dihydroxy-5-methoxycyclohexa-1,4-dien-1-yl)tridecan-2-yl acetate | |
0.00028 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | (2R)-1-(5-methoxy-3,6-dioxocyclohexa-1,4-dien-1-yl)pentadecan-2-yl acetate | |
0.00029 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | (2R)-1-(5-methoxy-3,6-dioxocyclohexa-1,4-dien-1-yl)tridecan-2-yl acetate | |
0.0021 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | 5-[(6Z)-13-(3,5-dihydroxy-4-methylcyclohexa-1,4-dien-1-yl)tridec-6-en-1-yl]benzene-1,3-diol | |
0.0021 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | (2R)-1-(5-methoxy-3,6-dioxocyclohexa-1,4-dien-1-yl)pentadecan-2-yl acetate | |
0.0023 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | 5-[(7Z)-15-(3-hydroxy-5-methoxyphenyl)pentadec-7-en-1-yl]-2-methylcyclohexa-1,4-diene-1,3-diol | |
0.0023 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | 5-[(8Z)-15-(3,5-dihydroxy-4-methylcyclohexa-1,4-dien-1-yl)pentadec-8-en-1-yl]benzene-1,3-diol | |
0.0025 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | 5-[(7Z)-13-(3-hydroxy-5-methoxyphenyl)tridec-7-en-1-yl]-2-methylcyclohexa-1,4-diene-1,3-diol | |
0.0027 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | 2-methyl-5-[(7Z)-pentadec-7-en-1-yl]cyclohexa-1,4-diene-1,3-diol | |
0.0028 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | 5-[(7Z)-tridec-7-en-1-yl]cyclohexa-1,4-diene-1,3-diol | |
0.0028 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | 5-[14-(3-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl)tetradecyl]benzene-1,3-diol | |
0.0029 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | 5-[(6Z)-13-(3-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl)tridec-6-en-1-yl]benzene-1,3-diol | |
0.0029 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | 5-[(7Z)-pentadec-7-en-1-yl]cyclohexa-1,4-diene-1,3-diol | |
0.0029 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | 5-[(8Z)-15-(3,5-dihydroxy-4-methylcyclohexa-1,4-dien-1-yl)pentadec-8-en-1-yl]-2-methylbenzene-1,3-diol | |
0.0029 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | 5-[(8Z)-15-(3-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl)pentadec-8-en-1-yl]benzene-1,3-diol | |
0.0029 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | (2R)-1-(3,6-dihydroxy-5-methoxycyclohexa-1,4-dien-1-yl)tridecan-2-yl acetate | |
0.0031 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | 5-[(6Z)-13-(3,5-dihydroxy-4-methylcyclohexa-1,4-dien-1-yl)tridec-6-en-1-yl]-2-methylbenzene-1,3-diol | |
0.0039 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | (2R)-1-(5-methoxy-3,6-dioxocyclohexa-1,4-dien-1-yl)tridecan-2-yl acetate | |
0.0047 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | 4-hydroxy-2-methoxy-6-(2-oxopentadecyl)cyclohexa-2,5-dien-1-yl acetate | |
0.0057 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | (2R)-1-[3-(acetyloxy)-6-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl]pentadecan-2-yl acetate | |
0.0076 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | 3-[(2S)-2-hydroxypentadecyl]-5-methoxycyclohexa-2,5-dien-1-ol | |
0.0096 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 5-[(6Z)-13-(3-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl)tridec-6-en-1-yl]benzene-1,3-diol | |
0.0117 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 5-[(6Z)-13-(3,5-dihydroxy-4-methylcyclohexa-1,4-dien-1-yl)tridec-6-en-1-yl]benzene-1,3-diol | |
0.0119 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 5-[(8Z)-15-(3,5-dihydroxy-4-methylcyclohexa-1,4-dien-1-yl)pentadec-8-en-1-yl]benzene-1,3-diol | |
0.0134 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 5-[(8Z)-15-(3-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl)pentadec-8-en-1-yl]benzene-1,3-diol | |
0.0139 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 5-[(6Z)-13-(3,5-dihydroxy-4-methylcyclohexa-1,4-dien-1-yl)tridec-6-en-1-yl]-2-methylbenzene-1,3-diol | |
0.0144 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 5-[14-(3-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl)tetradecyl]benzene-1,3-diol | |
0.0175 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 5-[(8Z)-15-(3,5-dihydroxy-4-methylcyclohexa-1,4-dien-1-yl)pentadec-8-en-1-yl]-2-methylbenzene-1,3-diol | |
0.0231 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | (2R)-1-(2-formyl-3,6-dihydroxy-5-methoxycyclohexa-1,4-dien-1-yl)tridecan-2-yl acetate | |
0.0251 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | (2R)-1-(2-hydroxy-5-methoxy-3,6-dioxocyclohexa-1,4-dien-1-yl)pentadecan-2-yl acetate | |
0.0317 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | (2R)-1-[3-(acetyloxy)-6-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl]tridecan-2-yl acetate | |
0.0325 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | 2-methoxy-6-tridecylcyclohexa-2,5-diene-1,4-dione | |
0.0367 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 5-[(7Z)-13-(3-hydroxy-5-methoxyphenyl)tridec-7-en-1-yl]-2-methylcyclohexa-1,4-diene-1,3-diol | |
0.041 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 4-hydroxy-2-methoxy-6-(2-oxopentadecyl)cyclohexa-2,5-dien-1-yl acetate | |
0.05 | - |
IC50 above 0.05 mM, isoform KGA, at pH 8.6 and 37°C | Homo sapiens | (2R)-1-(2-hydroxy-5-methoxy-3,6-dioxocyclohexa-1,4-dien-1-yl)pentadecan-2-yl acetate | |
0.05 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | (2R)-1-(2-hydroxy-5-methoxy-3,6-dioxocyclohexa-1,4-dien-1-yl)tridecan-2-yl acetate | |
0.05 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | (2S)-1-(5-methoxycyclohexa-1,4-dien-1-yl)heptan-2-ol | |
0.05 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | 2-hydroxy-5-methoxy-3-tridecylcyclohexa-2,5-diene-1,4-dione | |
0.05 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | 2-methoxy-6-pentadecylcyclohexa-2,5-diene-1,4-dione | |
0.05 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | 2-methyl-5-[(7Z)-tridec-7-en-1-yl]cyclohexa-1,4-diene-1,3-diol | |
0.05 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | (2R)-1-(2-formyl-3,6-dihydroxy-5-methoxycyclohexa-1,4-dien-1-yl)tridecan-2-yl acetate | |
0.05 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | (2R)-1-[3-(acetyloxy)-6-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl]tridecan-2-yl acetate | |
0.0524 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 3-[(2S)-2-hydroxypentadecyl]-5-methoxycyclohexa-2,5-dien-1-ol | |
0.0527 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | (2S)-1-(5-methoxycyclohexa-1,4-dien-1-yl)heptan-2-ol | |
0.0598 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 2-methyl-5-[(7Z)-tridec-7-en-1-yl]cyclohexa-1,4-diene-1,3-diol | |
0.0599 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 6-diazo-5-oxo-L-norleucine | |
0.0636 | - |
isoform GAB, at pH 8.6 and 37°C | Homo sapiens | bis-2-(5-phenylacetimido-1,2,4-thiadiazol-2-yl) ethyl sulfide | |
0.069 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | (2R)-1-[3-(acetyloxy)-6-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl]pentadecan-2-yl acetate | |
0.07 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 5-[(7Z)-15-(3-hydroxy-5-methoxyphenyl)pentadec-7-en-1-yl]-2-methylcyclohexa-1,4-diene-1,3-diol | |
0.073 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 5-[(7Z)-pentadec-7-en-1-yl]cyclohexa-1,4-diene-1,3-diol | |
0.0765 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 5-[(7Z)-tridec-7-en-1-yl]cyclohexa-1,4-diene-1,3-diol | |
0.0769 | - |
isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 2-methyl-5-[(7Z)-pentadec-7-en-1-yl]cyclohexa-1,4-diene-1,3-diol | |
0.5 | - |
IC50 above 0.05 mM, isoform KGA, at pH 8.6 and 37°C | Homo sapiens | (2R)-1-(2-hydroxy-5-methoxy-3,6-dioxocyclohexa-1,4-dien-1-yl)tridecan-2-yl acetate | |
0.5 | - |
IC50 above 0.05 mM, isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 2-hydroxy-5-methoxy-3-tridecylcyclohexa-2,5-diene-1,4-dione | |
0.5 | - |
IC50 above 0.05 mM, isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 2-methoxy-6-pentadecylcyclohexa-2,5-diene-1,4-dione | |
0.5 | - |
IC50 above 0.05 mM, isoform KGA, at pH 8.6 and 37°C | Homo sapiens | 2-methoxy-6-tridecylcyclohexa-2,5-diene-1,4-dione |
Organism | Comment | Expression |
---|---|---|
Homo sapiens | isoforms GAB and KGA protein expression levels are higher in human hepatoma HepG2 and lung carcinoma A549 cells than those in fibroblast cell lines Detroit 551 and WI-38, whilst isoform GAC expression levels are not significantly changed | up |