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Literature summary for 3.5.1.2 extracted from

  • Lee, Y.Z.; Yang, C.W.; Chang, H.Y.; Hsu, H.Y.; Chen, I.S.; Chang, H.S.; Lee, C.H.; Lee, J.C.; Kumar, C.R.; Qiu, Y.Q.; Chao, Y.S.; Lee, S.J.
    Discovery of selective inhibitors of glutaminase-2, which inhibit mTORC1, activate autophagy and inhibit proliferation in cancer cells (2014), Oncotarget, 5, 6087-6101.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli C41(DE3)pLysS cells Homo sapiens

Protein Variants

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

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/ 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
-
-
-

Purification (Commentary)

Purification (Comment) Organism
Ni+-charged affinity column chromatography Homo sapiens

Source Tissue

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 and Products (Substrate)

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

Synonyms

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 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

Expression

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