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8SZJ
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BU of 8szj by Molmil
Human glutaminase C (Y466W) with L-Gln and Pi, filamentous form
Descriptor: GLUTAMINE, Glutaminase kidney isoform, mitochondrial, ...
Authors:Feng, S, Aplin, C, Nguyen, T.-T.T, Milano, S.K, Cerione, R.A.
Deposit date:2023-05-29
Release date:2024-03-13
Method:ELECTRON MICROSCOPY (3.35 Å)
Cite:Filament formation drives catalysis by glutaminase enzymes important in cancer progression.
Nat Commun, 15, 2024
8T0Z
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BU of 8t0z by Molmil
Human liver-type glutaminase (K253A) with L-Gln, filamentous form
Descriptor: GLUTAMINE, Glutaminase liver isoform, mitochondrial
Authors:Feng, S, Aplin, C, Nguyen, T.-T.T, Milano, S.K, Cerione, R.A.
Deposit date:2023-06-01
Release date:2024-03-13
Method:ELECTRON MICROSCOPY (3.3 Å)
Cite:Filament formation drives catalysis by glutaminase enzymes important in cancer progression.
Nat Commun, 15, 2024
8SZL
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BU of 8szl by Molmil
Human liver-type glutaminase (Apo form)
Descriptor: Glutaminase liver isoform, mitochondrial
Authors:Feng, S, Aplin, C, Nguyen, T.-T.T, Milano, S.K, Cerione, R.A.
Deposit date:2023-05-30
Release date:2024-03-13
Method:ELECTRON MICROSCOPY (3.12 Å)
Cite:Filament formation drives catalysis by glutaminase enzymes important in cancer progression.
Nat Commun, 15, 2024
8JUB
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BU of 8jub by Molmil
Crystal structure of glutaminase C in complex with compound 27
Descriptor: 3-[2-oxidanylidene-2-[[5-[[(3R)-1-pyridazin-3-ylpyrrolidin-3-yl]amino]-1,3,4-thiadiazol-2-yl]amino]ethyl]benzoic acid, Glutaminase kidney isoform, mitochondrial
Authors:Wang, X, Hanyu, S, Tingting, D.
Deposit date:2023-06-26
Release date:2023-10-11
Last modified:2023-11-01
Method:X-RAY DIFFRACTION (2.01 Å)
Cite:Targeting the Subpocket Enables the Discovery of Thiadiazole-Pyridazine Derivatives as Glutaminase C Inhibitors.
Acs Med.Chem.Lett., 14, 2023
8JUE
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BU of 8jue by Molmil
Crystal structure of glutaminase C in complex with compound 11
Descriptor: 2-(3-phenoxyphenyl)-N-[5-[[(3R)-1-pyridazin-3-ylpyrrolidin-3-yl]amino]-1,3,4-thiadiazol-2-yl]ethanamide, Glutaminase kidney isoform, mitochondrial
Authors:Wang, X, Hanyu, S, Tingting, D.
Deposit date:2023-06-26
Release date:2023-10-11
Last modified:2023-11-01
Method:X-RAY DIFFRACTION (2.39 Å)
Cite:Targeting the Subpocket Enables the Discovery of Thiadiazole-Pyridazine Derivatives as Glutaminase C Inhibitors.
Acs Med.Chem.Lett., 14, 2023
8EC6
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BU of 8ec6 by Molmil
Cryo-EM structure of the Glutaminase C core filament (fGAC)
Descriptor: Isoform 2 of Glutaminase kidney isoform, mitochondrial, PHOSPHATE ION
Authors:Ambrosio, A.L, Dias, S.M, Quesnay, J.E, Portugal, R.V, Cassago, A, van Heel, M.G, Islam, Z, Rodrigues, C.T.
Deposit date:2022-09-01
Release date:2023-09-20
Last modified:2023-12-27
Method:ELECTRON MICROSCOPY (3.1 Å)
Cite:Molecular mechanism of glutaminase activation through filamentation and the role of filaments in mitophagy protection.
Nat.Struct.Mol.Biol., 30, 2023
8BSK
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BU of 8bsk by Molmil
Human GLS in complex with compound 3
Descriptor: Glutaminase kidney isoform, mitochondrial 65 kDa chain, N,N'-[sulfanediylbis(ethane-2,1-diyl-1,3,4-thiadiazole-5,2-diyl)]bis(2-phenylacetamide), ...
Authors:Debreczeni, J.E.
Deposit date:2022-11-25
Release date:2023-01-18
Method:X-RAY DIFFRACTION (2.1 Å)
Cite:Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models.
J Med Chem, 62, 2019
8BSL
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BU of 8bsl by Molmil
Human GLS in complex with compound 12
Descriptor: Glutaminase kidney isoform, mitochondrial, ~{N}-[5-[[(3~{R})-1-(5-azanyl-1,3,4-thiadiazol-2-yl)pyrrolidin-3-yl]amino]-1,3,4-thiadiazol-2-yl]-2-phenyl-ethanamide
Authors:Debreczeni, J.E.
Deposit date:2022-11-25
Release date:2023-01-18
Method:X-RAY DIFFRACTION (2.38 Å)
Cite:Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models.
J Med Chem, 62, 2019
8BSM
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BU of 8bsm by Molmil
Human GLS in complex with compound 18
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 65 kDa chain, ...
Authors:Debreczeni, J.E.
Deposit date:2022-11-25
Release date:2023-01-18
Method:X-RAY DIFFRACTION (2.782 Å)
Cite:Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models.
J Med Chem, 62, 2019
8BSN
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BU of 8bsn by Molmil
Human GLS in complex with compound 27
Descriptor: (2~{S})-2-methoxy-2-phenyl-~{N}-[5-[[(3~{R})-1-pyridazin-3-ylpyrrolidin-3-yl]amino]-1,3,4-thiadiazol-2-yl]ethanamide, Glutaminase kidney isoform, mitochondrial 65 kDa chain, ...
Authors:Debreczeni, J.E.
Deposit date:2022-11-25
Release date:2023-01-18
Method:X-RAY DIFFRACTION (2.494 Å)
Cite:Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models.
J Med Chem, 62, 2019
8GWR
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BU of 8gwr by Molmil
Near full length Kidney type Glutaminase in complex with 2,2-Dimethyl-2,3-Dihydrobenzo[a] Phenanthridin-4(1H)-one (DDP)
Descriptor: 2,2-dimethyl-1,3-dihydrobenzo[a]phenanthridin-4-one, Glutaminase kidney isoform, mitochondrial
Authors:Shankar, S, Jobichen, C, Sivaraman, J.
Deposit date:2022-09-17
Release date:2022-12-21
Last modified:2023-11-29
Method:X-RAY DIFFRACTION (2.801 Å)
Cite:A novel allosteric site employs a conserved inhibition mechanism in human kidney-type glutaminase.
Febs J., 290, 2023
7REN
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BU of 7ren by Molmil
Room temperature serial crystal structure of Glutaminase C in complex with inhibitor 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:Milano, S.K, Finke, A, Cerione, R.A.
Deposit date:2021-07-13
Release date:2022-05-25
Last modified:2023-10-18
Method:X-RAY DIFFRACTION (2.8 Å)
Cite:New insights into the molecular mechanisms of glutaminase C inhibitors in cancer cells using serial room temperature crystallography.
J.Biol.Chem., 298, 2022
7RGG
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BU of 7rgg by Molmil
Room temperature serial crystal structure of Glutaminase C in complex with inhibitor BPTES
Descriptor: Glutaminase kidney isoform, mitochondrial 68 kDa chain, N,N'-[sulfanediylbis(ethane-2,1-diyl-1,3,4-thiadiazole-5,2-diyl)]bis(2-phenylacetamide)
Authors:Milano, S.K, Finke, A, Cerione, R.A.
Deposit date:2021-07-15
Release date:2022-05-25
Last modified:2023-10-18
Method:X-RAY DIFFRACTION (3 Å)
Cite:New insights into the molecular mechanisms of glutaminase C inhibitors in cancer cells using serial room temperature crystallography.
J.Biol.Chem., 298, 2022
7SBN
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BU of 7sbn by Molmil
Human glutaminase C (Y466W) with L-Gln, closed conformation
Descriptor: GLUTAMINE, Isoform 3 of Glutaminase kidney isoform, mitochondrial
Authors:Nguyen, T.-T.T, Cerione, R.A.
Deposit date:2021-09-25
Release date:2022-02-02
Last modified:2023-10-18
Method:X-RAY DIFFRACTION (2.14 Å)
Cite:High-resolution structures of mitochondrial glutaminase C tetramers indicate conformational changes upon phosphate binding.
J.Biol.Chem., 298, 2022
7SBM
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BU of 7sbm by Molmil
Human glutaminase C (Y466W) with L-Gln, open conformation
Descriptor: GLUTAMINE, Isoform 3 of Glutaminase kidney isoform, mitochondrial
Authors:Nguyen, T.-T.T, Cerione, R.A.
Deposit date:2021-09-25
Release date:2022-02-02
Last modified:2023-10-18
Method:X-RAY DIFFRACTION (2.8 Å)
Cite:High-resolution structures of mitochondrial glutaminase C tetramers indicate conformational changes upon phosphate binding.
J.Biol.Chem., 298, 2022
6LOX
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BU of 6lox by Molmil
Crystal Structure of human glutaminase with macrocyclic inhibitor
Descriptor: (E)-15,22-Dioxa-4,11-diaza-5(2,5)-thiadiazola-10(3,6)-pyridazina-1,14(1,3)-dibenzenacyclodocosaphan-18-ene-3,12-dione, Glutaminase kidney isoform, mitochondrial
Authors:Bian, J, Li, Z, Xu, X, Wang, J, Li, L.
Deposit date:2020-01-07
Release date:2021-01-13
Last modified:2023-11-29
Method:X-RAY DIFFRACTION (3.2 Å)
Cite:Structure-Enabled Discovery of Novel Macrocyclic Inhibitors Targeting Glutaminase 1 Allosteric Binding Site.
J.Med.Chem., 64, 2021
6UMD
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BU of 6umd by Molmil
Crystal structure of human GAC in complex with inhibitor UPGL00012
Descriptor: 2-(pyridin-3-yl)-N-(5-{4-[(5-{[(pyridin-3-yl)acetyl]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:2019-10-09
Release date:2020-10-14
Last modified:2023-10-11
Method:X-RAY DIFFRACTION (2.7 Å)
Cite:Crystal structure of human GAC in complex with inhibitor UPGL00012
To Be Published
6UME
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BU of 6ume by Molmil
Crystal structure of human GAC in complex with inhibitor UPGL00012
Descriptor: 2-(pyridin-3-yl)-N-(5-{4-[(5-{[(pyridin-3-yl)acetyl]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:2019-10-09
Release date:2020-10-14
Last modified:2023-10-11
Method:X-RAY DIFFRACTION (2.9 Å)
Cite:Crystal structure of human GAC in complex with inhibitor UPGL00012
To Be Published
6UMC
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BU of 6umc by Molmil
Crystal structure of human GAC in complex with inhibitor UPGL00012
Descriptor: 2-phenyl-N-{5-[(3R)-3-({5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl}oxy)pyrrolidin-1-yl]-1,3,4-thiadiazol-2-yl}acetamide, Glutaminase kidney isoform, mitochondrial
Authors:Huang, Q, Cerione, R.A.
Deposit date:2019-10-09
Release date:2020-10-14
Last modified:2023-10-11
Method:X-RAY DIFFRACTION (2.75 Å)
Cite:Crystal structure of human GAC in complex with inhibitor UPGL00012
To Be Published
6ULJ
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BU of 6ulj by Molmil
Crystal structure of human GAC in complex with inhibitor UPGL00012
Descriptor: 2-phenyl-N-{6-[4-({6-[(phenylacetyl)amino]pyridazin-3-yl}oxy)piperidin-1-yl]pyridazin-3-yl}acetamide, Glutaminase kidney isoform, mitochondrial
Authors:Huang, Q, Cerione, R.A.
Deposit date:2019-10-08
Release date:2020-10-14
Last modified:2023-10-11
Method:X-RAY DIFFRACTION (2.69 Å)
Cite:Crystal structure of human GAC in complex with inhibitor UPGL00045
To Be Published
6UMF
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BU of 6umf by Molmil
Crystal structure of human GAC in complex with inhibitor UPGL00012
Descriptor: Glutaminase kidney isoform, mitochondrial, N-(5-{[1-(5-amino-1,3,4-thiadiazol-2-yl)piperidin-4-yl]oxy}-1,3,4-thiadiazol-2-yl)-2-phenylacetamide
Authors:Huang, Q, Cerione, R.A.
Deposit date:2019-10-09
Release date:2020-10-14
Last modified:2023-10-11
Method:X-RAY DIFFRACTION (2.68 Å)
Cite:Crystal structure of human GAC in complex with inhibitor UPGL00012
To Be Published
6ULA
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BU of 6ula by Molmil
Crystal structure of human GAC in complex with inhibitor UPGL00012
Descriptor: 2-cyclopropyl-N-{5-[4-({5-[(cyclopropylacetyl)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.A.
Deposit date:2019-10-07
Release date:2020-10-14
Last modified:2023-10-11
Method:X-RAY DIFFRACTION (2.95 Å)
Cite:Crystal structure of human GAC in complex with inhibitor UPGL00030
To Be Published
6UL9
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BU of 6ul9 by Molmil
Crystal structure of human GAC in complex with inhibitor UPGL00023
Descriptor: 2-phenyl-N-{5-[(1-{5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl}azetidin-3-yl)oxy]-1,3,4-thiadiazol-2-yl}acetamide, Glutaminase kidney isoform, mitochondrial
Authors:Huang, Q.Q, Cerione, R.A.
Deposit date:2019-10-07
Release date:2020-10-14
Last modified:2023-10-11
Method:X-RAY DIFFRACTION (2.5 Å)
Cite:Crystal structure of human GAC in complex with inhibitor UPGL00012
To Be Published
6UJG
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BU of 6ujg by Molmil
Crystal structure of human GAC in complex with inhibitor UPGL00012
Descriptor: Glutaminase kidney isoform, mitochondrial, N-{5-[(3S)-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 (3 Å)
Cite:Crystal structure of human GAC in complex with inhibitor UPGL00012
To Be Published
6UK6
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BU of 6uk6 by Molmil
Crystal structure of human GAC in complex with inhibitor UPGL00018
Descriptor: 5-{4-[(5-amino-1,3,4-thiadiazol-2-yl)oxy]piperidin-1-yl}-1,3,4-thiadiazol-2-amine, Glutaminase kidney isoform, mitochondrial
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 (2.9 Å)
Cite:Crystal structure of human GAC in complex with inhibitor UPGL00018
To Be Published

 

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PDB entries from 2024-03-27

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