8JUB
 
 | | Crystal structure of glutaminase C in complex with compound 27 | | 分子名称: | 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 | | 著者 | Wang, X, Hanyu, S, Tingting, D. | | 登録日 | 2023-06-26 | | 公開日 | 2023-10-11 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (2.01 Å) | | 主引用文献 | Targeting the Subpocket Enables the Discovery of Thiadiazole-Pyridazine Derivatives as Glutaminase C Inhibitors.
Acs Med.Chem.Lett., 14, 2023
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8JUE
 | | Crystal structure of glutaminase C in complex with compound 11 | | 分子名称: | 2-(3-phenoxyphenyl)-N-[5-[[(3R)-1-pyridazin-3-ylpyrrolidin-3-yl]amino]-1,3,4-thiadiazol-2-yl]ethanamide, Glutaminase kidney isoform, mitochondrial | | 著者 | Wang, X, Hanyu, S, Tingting, D. | | 登録日 | 2023-06-26 | | 公開日 | 2023-10-11 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (2.39 Å) | | 主引用文献 | Targeting the Subpocket Enables the Discovery of Thiadiazole-Pyridazine Derivatives as Glutaminase C Inhibitors.
Acs Med.Chem.Lett., 14, 2023
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8T0Z
 | | Human liver-type glutaminase (K253A) with L-Gln, filamentous form | | 分子名称: | GLUTAMINE, Glutaminase liver isoform, mitochondrial | | 著者 | Feng, S, Aplin, C, Nguyen, T.-T.T, Milano, S.K, Cerione, R.A. | | 登録日 | 2023-06-01 | | 公開日 | 2024-03-13 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | Filament formation drives catalysis by glutaminase enzymes important in cancer progression.
Nat Commun, 15, 2024
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8SZL
 | | Human liver-type glutaminase (Apo form) | | 分子名称: | Glutaminase liver isoform, mitochondrial | | 著者 | Feng, S, Aplin, C, Nguyen, T.-T.T, Milano, S.K, Cerione, R.A. | | 登録日 | 2023-05-30 | | 公開日 | 2024-03-13 | | 実験手法 | ELECTRON MICROSCOPY (3.12 Å) | | 主引用文献 | Filament formation drives catalysis by glutaminase enzymes important in cancer progression.
Nat Commun, 15, 2024
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8SZJ
 | | Human glutaminase C (Y466W) with L-Gln and Pi, filamentous form | | 分子名称: | GLUTAMINE, Glutaminase kidney isoform, mitochondrial, ... | | 著者 | Feng, S, Aplin, C, Nguyen, T.-T.T, Milano, S.K, Cerione, R.A. | | 登録日 | 2023-05-29 | | 公開日 | 2024-03-13 | | 実験手法 | ELECTRON MICROSCOPY (3.35 Å) | | 主引用文献 | Filament formation drives catalysis by glutaminase enzymes important in cancer progression.
Nat Commun, 15, 2024
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8BSK
 | | Human GLS in complex with compound 3 | | 分子名称: | Glutaminase kidney isoform, mitochondrial 65 kDa chain, N,N'-[sulfanediylbis(ethane-2,1-diyl-1,3,4-thiadiazole-5,2-diyl)]bis(2-phenylacetamide), ... | | 著者 | Debreczeni, J.E. | | 登録日 | 2022-11-25 | | 公開日 | 2023-01-18 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | 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
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8BSL
 | | Human GLS in complex with compound 12 | | 分子名称: | 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 | | 著者 | Debreczeni, J.E. | | 登録日 | 2022-11-25 | | 公開日 | 2023-01-18 | | 実験手法 | X-RAY DIFFRACTION (2.38 Å) | | 主引用文献 | 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
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8BSM
 | | Human GLS in complex with compound 18 | | 分子名称: | 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, ... | | 著者 | Debreczeni, J.E. | | 登録日 | 2022-11-25 | | 公開日 | 2023-01-18 | | 実験手法 | X-RAY DIFFRACTION (2.782 Å) | | 主引用文献 | 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
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8BSN
 | | Human GLS in complex with compound 27 | | 分子名称: | (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, ... | | 著者 | Debreczeni, J.E. | | 登録日 | 2022-11-25 | | 公開日 | 2023-01-18 | | 実験手法 | X-RAY DIFFRACTION (2.494 Å) | | 主引用文献 | 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
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8GWR
 | | Near full length Kidney type Glutaminase in complex with 2,2-Dimethyl-2,3-Dihydrobenzo[a] Phenanthridin-4(1H)-one (DDP) | | 分子名称: | 2,2-dimethyl-1,3-dihydrobenzo[a]phenanthridin-4-one, Glutaminase kidney isoform, mitochondrial | | 著者 | Shankar, S, Jobichen, C, Sivaraman, J. | | 登録日 | 2022-09-17 | | 公開日 | 2022-12-21 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (2.801 Å) | | 主引用文献 | A novel allosteric site employs a conserved inhibition mechanism in human kidney-type glutaminase.
Febs J., 290, 2023
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8EC6
 | | Cryo-EM structure of the Glutaminase C core filament (fGAC) | | 分子名称: | Isoform 2 of Glutaminase kidney isoform, mitochondrial, PHOSPHATE ION | | 著者 | Ambrosio, A.L, Dias, S.M, Quesnay, J.E, Portugal, R.V, Cassago, A, van Heel, M.G, Islam, Z, Rodrigues, C.T. | | 登録日 | 2022-09-01 | | 公開日 | 2023-09-20 | | 最終更新日 | 2023-12-27 | | 実験手法 | ELECTRON MICROSCOPY (3.1 Å) | | 主引用文献 | Molecular mechanism of glutaminase activation through filamentation and the role of filaments in mitophagy protection.
Nat.Struct.Mol.Biol., 30, 2023
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7SBM
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7SBN
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7RGG
 | | Room temperature serial crystal structure of Glutaminase C in complex with inhibitor BPTES | | 分子名称: | Glutaminase kidney isoform, mitochondrial 68 kDa chain, N,N'-[sulfanediylbis(ethane-2,1-diyl-1,3,4-thiadiazole-5,2-diyl)]bis(2-phenylacetamide) | | 著者 | Milano, S.K, Finke, A, Cerione, R.A. | | 登録日 | 2021-07-15 | | 公開日 | 2022-05-25 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | New insights into the molecular mechanisms of glutaminase C inhibitors in cancer cells using serial room temperature crystallography.
J.Biol.Chem., 298, 2022
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7REN
 | | Room temperature serial crystal structure of Glutaminase C in complex with inhibitor UPGL-00004 | | 分子名称: | 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 | | 著者 | Milano, S.K, Finke, A, Cerione, R.A. | | 登録日 | 2021-07-13 | | 公開日 | 2022-05-25 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | New insights into the molecular mechanisms of glutaminase C inhibitors in cancer cells using serial room temperature crystallography.
J.Biol.Chem., 298, 2022
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6LOX
 | | Crystal Structure of human glutaminase with macrocyclic inhibitor | | 分子名称: | (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 | | 著者 | Bian, J, Li, Z, Xu, X, Wang, J, Li, L. | | 登録日 | 2020-01-07 | | 公開日 | 2021-01-13 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Structure-Enabled Discovery of Novel Macrocyclic Inhibitors Targeting Glutaminase 1 Allosteric Binding Site.
J.Med.Chem., 64, 2021
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6UMD
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6UME
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6UMC
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6UMF
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6ULJ
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6ULA
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6UL9
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6UK6
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6UKB
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