6UKB
| Crystal structure of human GAC in complex with inhibitor UPGL00012 | Descriptor: | Glutaminase kidney isoform, mitochondrial, N-[5-(4-{[5-(acetylamino)-1,3,4-thiadiazol-2-yl]oxy}piperidin-1-yl)-1,3,4-thiadiazol-2-yl]acetamide | Authors: | Huang, Q, Cerione, R.A. | Deposit date: | 2019-10-04 | Release date: | 2020-10-07 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (3 Å) | Cite: | Crystal structure of human GAC in complex with inhibitor UPGL00020 To Be Published
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6UJM
| Crystal structure of human GAC in complex with inhibitor UPGL00013 | Descriptor: | Glutaminase kidney isoform, mitochondrial, N-{5-[(3R)-3-{[5-(acetylamino)-1,3,4-thiadiazol-2-yl]amino}pyrrolidin-1-yl]-1,3,4-thiadiazol-2-yl}acetamide | Authors: | Huang, Q, Cerione, R.A. | Deposit date: | 2019-10-03 | Release date: | 2020-10-07 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Crystal structure of human GAC in complex with inhibitor UPGL00013 To Be Published
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5W2J
| Crystal structure of dimeric form of mouse Glutaminase C | Descriptor: | CHLORIDE ION, Glutaminase kidney isoform, mitochondrial, ... | Authors: | Cerione, R.A, Li, Y. | Deposit date: | 2017-06-06 | Release date: | 2018-10-17 | Last modified: | 2024-03-13 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Mechanistic Basis of Glutaminase Activation: A KEY ENZYME THAT PROMOTES GLUTAMINE METABOLISM IN CANCER CELLS. J. Biol. Chem., 291, 2016
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5WJ6
| Crystal structure of glutaminase C in complex with inhibitor 2-phenyl-N-{5-[4-({5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl}amino)piperidin-1-yl]-1,3,4-thiadiazol-2-yl}acetamide (UPGL-00004) | Descriptor: | 2-phenyl-N-{5-[4-({5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl}amino)piperidin-1-yl]-1,3,4-thiadiazol-2-yl}acetamide, Glutaminase kidney isoform, mitochondrial | Authors: | Huang, Q, Cerione, R.A. | Deposit date: | 2017-07-21 | Release date: | 2018-01-10 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.445 Å) | Cite: | Characterization of the interactions of potent allosteric inhibitors with glutaminase C, a key enzyme in cancer cell glutamine metabolism. J. Biol. Chem., 293, 2018
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5UQE
| Multidomain structure of human kidney-type glutaminase(KGA/GLS) | Descriptor: | Glutaminase kidney isoform, mitochondrial, N,N'-[sulfanediylbis(ethane-2,1-diyl-1,3,4-thiadiazole-5,2-diyl)]bis(2-phenylacetamide) | Authors: | Pasquali, C.C, Dias, S.M.G, Ambrosio, A.L.B. | Deposit date: | 2017-02-08 | Release date: | 2017-05-24 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (3.6 Å) | Cite: | The origin and evolution of human glutaminases and their atypical C-terminal ankyrin repeats. J. Biol. Chem., 292, 2017
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5HL1
| Crystal structure of glutaminase C in complex with inhibitor CB-839 | Descriptor: | 2-(pyridin-2-yl)-N-(5-{4-[6-({[3-(trifluoromethoxy)phenyl]acetyl}amino)pyridazin-3-yl]butyl}-1,3,4-thiadiazol-2-yl)acetamide, Glutaminase kidney isoform, mitochondrial | Authors: | Huang, Q, Cerione, R.A. | Deposit date: | 2016-01-14 | Release date: | 2016-08-24 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | Crystal structure of the clinically relevant glutaminase inhibitot CB-839 in complex with glutaminase C To Be Published
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5JYO
| Allosteric inhibition of Kidney Isoform of Glutaminase | Descriptor: | 2-(pyridin-2-yl)-N-(5-{4-[6-({[3-(trifluoromethoxy)phenyl]acetyl}amino)pyridazin-3-yl]butyl}-1,3,4-thiadiazol-2-yl)acetamide, Glutaminase kidney isoform, mitochondrial | Authors: | Sivaraman, J, Jayaraman, S. | Deposit date: | 2016-05-15 | Release date: | 2016-08-03 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (2.098 Å) | Cite: | Structural basis for exploring the allosteric inhibition of human kidney type glutaminase. Oncotarget, 7, 2016
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5JYP
| Allosteric inhibition of Kidney Isoform of Glutaminase | Descriptor: | 2-phenyl-~{N}-[5-[(1~{S},3~{S})-3-[5-(2-phenylethanoylamino)-1,3,4-thiadiazol-2-yl]cyclohexyl]-1,3,4-thiadiazol-2-yl]ethanamide, Glutaminase kidney isoform, mitochondrial | Authors: | Ramachandran, S, Sivaraman, J. | Deposit date: | 2016-05-15 | Release date: | 2016-08-03 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (2.74 Å) | Cite: | Structural basis for exploring the allosteric inhibition of human kidney type glutaminase. Oncotarget, 7, 2016
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5I94
| Crystal structure of human glutaminase C in complex with the inhibitor UPGL-00019 | Descriptor: | 2-phenyl-N-{5-[4-({5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl}oxy)piperidin-1-yl]-1,3,4-thiadiazol-2-yl}acetamide, Glutaminase kidney isoform, mitochondrial | Authors: | Huang, Q, Cerione, R. | Deposit date: | 2016-02-19 | Release date: | 2016-05-11 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.983 Å) | Cite: | Design and evaluation of novel glutaminase inhibitors. Bioorg.Med.Chem., 24, 2016
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5FI7
| Crystal structure of human GAC in complex with inhibitor UPGL_00015: 2-phenyl-~{N}-[5-[(3~{S})-3-[[5-(2-phenylethanoylamino)-1,3,4-thiadiazol-2-yl]oxy]pyrrolidin-1-yl]-1,3,4-thiadiazol-2-yl]ethanamide | Descriptor: | 2-phenyl-~{N}-[5-[(3~{S})-3-[[5-(2-phenylethanoylamino)-1,3,4-thiadiazol-2-yl]oxy]pyrrolidin-1-yl]-1,3,4-thiadiazol-2-yl]ethanamide, Glutaminase kidney isoform, mitochondrial | Authors: | Huang, Q, Cerione, R. | Deposit date: | 2015-12-22 | Release date: | 2016-05-11 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Design and evaluation of novel glutaminase inhibitors. Bioorg.Med.Chem., 24, 2016
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5FI2
| Crystal structure of human GAC in complex with inhibitor UPGL_00009: 2-phenyl-~{N}-[5-[[(3~{R})-1-[5-(2-phenylethanoylamino)-1,3,4-thiadiazol- 2-yl]pyrrolidin-3-yl]amino]-1,3,4-thiadiazol-2-yl]ethanamide | Descriptor: | 2-phenyl-~{N}-[5-[[(3~{R})-1-[5-(2-phenylethanoylamino)-1,3,4-thiadiazol-2-yl]pyrrolidin-3-yl]amino]-1,3,4-thiadiazol-2-yl]ethanamide, Glutaminase kidney isoform, mitochondrial | Authors: | Huang, Q, Cerione, R. | Deposit date: | 2015-12-22 | Release date: | 2016-05-11 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Design and evaluation of novel glutaminase inhibitors. Bioorg.Med.Chem., 24, 2016
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5FI6
| Crystal structure of human GAC in complex with inhibitor UPGL_00011: 2-phenyl-~{N}-[5-[[(3~{S})-1-[5-(2-phenylethanoylamino)-1,3,4-thiadiazol-2-yl]pyrrolidin-3-yl]amino]-1,3,4-thiadiazol-2-yl]ethanamide | Descriptor: | 2-phenyl-~{N}-[5-[[(3~{S})-1-[5-(2-phenylethanoylamino)-1,3,4-thiadiazol-2-yl]pyrrolidin-3-yl]amino]-1,3,4-thiadiazol-2-yl]ethanamide, Glutaminase kidney isoform, mitochondrial | Authors: | Huang, Q, Cerione, R. | Deposit date: | 2015-12-22 | Release date: | 2016-05-11 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (2.52 Å) | Cite: | Design and evaluation of novel glutaminase inhibitors. Bioorg.Med.Chem., 24, 2016
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5D3O
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4O7D
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4JKT
| Crystal structure of mouse Glutaminase C, BPTES-bound form | Descriptor: | Glutaminase kidney isoform, mitochondrial, N,N'-[sulfanediylbis(ethane-2,1-diyl-1,3,4-thiadiazole-5,2-diyl)]bis(2-phenylacetamide) | Authors: | Fornezari, C, Ferreira, A.P.S, Dias, S.M.G, Ambrosio, A.L.B. | Deposit date: | 2013-03-11 | Release date: | 2013-08-14 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.77 Å) | Cite: | Active Glutaminase C Self-assembles into a Supratetrameric Oligomer That Can Be Disrupted by an Allosteric Inhibitor. J.Biol.Chem., 288, 2013
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4BQM
| Crystal structure of human liver-type glutaminase, catalytic domain | Descriptor: | 1,2-ETHANEDIOL, CHLORIDE ION, GLUTAMINASE LIVER ISOFORM, ... | Authors: | Ferreira, I.M, Vollmar, M, Krojer, T, Strain-Damerell, C, Froese, S, Coutandin, D, Williams, E, Burgess-Brown, N, von Delft, F, Arrowsmith, C.H, Bountra, C, Edwards, A, Dias, S.M.G, Ambrosio, A.L.B, Yue, W.W. | Deposit date: | 2013-05-31 | Release date: | 2013-07-10 | Last modified: | 2023-12-20 | Method: | X-RAY DIFFRACTION (2.18 Å) | Cite: | Crystal Structure of Human Liver-Type Glutaminase, Catalytic Domain To be Published
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3VP0
| Crystal structure of human glutaminase in complex with L-glutamine | Descriptor: | GLUTAMINE, Glutaminase kidney isoform, mitochondrial, ... | Authors: | Thangavelu, K, Sivaraman, J. | Deposit date: | 2012-02-23 | Release date: | 2012-06-13 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | Structural basis for the allosteric inhibitory mechanism of human kidney-type glutaminase (KGA) and its regulation by Raf-Mek-Erk signaling in cancer cell metabolism. Proc.Natl.Acad.Sci.USA, 109, 2012
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3VP2
| Crystal structure of human glutaminase in complex with inhibitor 2 | Descriptor: | 5,5'-(sulfanediyldiethane-2,1-diyl)bis(1,3,4-thiadiazol-2-amine), Glutaminase kidney isoform, mitochondrial, ... | Authors: | Thangavelu, K, Sivaraman, J. | Deposit date: | 2012-02-23 | Release date: | 2012-06-13 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Structural basis for the allosteric inhibitory mechanism of human kidney-type glutaminase (KGA) and its regulation by Raf-Mek-Erk signaling in cancer cell metabolism. Proc.Natl.Acad.Sci.USA, 109, 2012
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3VOZ
| Crystal structure of human glutaminase in complex with BPTES | Descriptor: | Glutaminase kidney isoform, mitochondrial, N,N'-[sulfanediylbis(ethane-2,1-diyl-1,3,4-thiadiazole-5,2-diyl)]bis(2-phenylacetamide), ... | Authors: | Thangavelu, K, Sivaraman, J. | Deposit date: | 2012-02-23 | Release date: | 2012-06-13 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | Structural basis for the allosteric inhibitory mechanism of human kidney-type glutaminase (KGA) and its regulation by Raf-Mek-Erk signaling in cancer cell metabolism. Proc.Natl.Acad.Sci.USA, 109, 2012
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3VOY
| Crystal structure of human glutaminase in apo form | Descriptor: | Glutaminase kidney isoform, mitochondrial, SULFATE ION | Authors: | Thangavelu, K, Sivaraman, J. | Deposit date: | 2012-02-23 | Release date: | 2012-06-13 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Structural basis for the allosteric inhibitory mechanism of human kidney-type glutaminase (KGA) and its regulation by Raf-Mek-Erk signaling in cancer cell metabolism. Proc.Natl.Acad.Sci.USA, 109, 2012
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3VP3
| Crystal structure of human glutaminase in complex with inhibitor 3 | Descriptor: | 5,5'-pentane-1,5-diylbis(1,3,4-thiadiazol-2-amine), Glutaminase kidney isoform, mitochondrial, ... | Authors: | Thangavelu, K, Sivaraman, J. | Deposit date: | 2012-02-23 | Release date: | 2012-06-13 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Structural basis for the allosteric inhibitory mechanism of human kidney-type glutaminase (KGA) and its regulation by Raf-Mek-Erk signaling in cancer cell metabolism. Proc.Natl.Acad.Sci.USA, 109, 2012
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3VP4
| Crystal structure of human glutaminase in complex with inhibitor 4 | Descriptor: | 5,5'-butane-1,4-diylbis(1,3,4-thiadiazol-2-amine), Glutaminase kidney isoform, mitochondrial | Authors: | Thangavelu, K, Sivaraman, J. | Deposit date: | 2012-02-23 | Release date: | 2012-06-13 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (2.45 Å) | Cite: | Structural basis for the allosteric inhibitory mechanism of human kidney-type glutaminase (KGA) and its regulation by Raf-Mek-Erk signaling in cancer cell metabolism. Proc.Natl.Acad.Sci.USA, 109, 2012
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3VP1
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3SS5
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3SS4
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