3ZUN
 
 | | pVHL54-213-EloB-EloC complex_(2S,4R)-4-hydroxy-1-(2-(3-methylisoxazol- 5-yl)acetyl)-N-(4-nitrobenzyl)pyrrolidine-2-carboxamide bound | | Descriptor: | (4R)-N-[4-(DIHYDROXYAMINO)BENZYL]-4-HYDROXY-1-[(3-METHYLISOXAZOL-5-YL)ACETYL]-L-PROLINAMIDE, GLYCEROL, TRANSCRIPTION ELONGATION FACTOR B POLYPEPTIDE 1, ... | | Authors: | Van Molle, I, Buckley, D, Crews, C.M, Ciulli, A. | | Deposit date: | 2011-07-19 | | Release date: | 2012-07-25 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Elongin-B, Elongin-C, Von Hippel-Lindau Disease Tumor Suppressor Complex
To be Published
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3ZKJ
 | | Crystal Structure of Ankyrin Repeat and Socs Box-Containing Protein 9 (Asb9) in Complex with Elonginb and Elonginc | | Descriptor: | 1,2-ETHANEDIOL, ANKYRIN REPEAT AND SOCS BOX PROTEIN 9, CHLORIDE ION, ... | | Authors: | Muniz, J.R.C, Guo, K, Zhang, Y, Ayinampudi, V, Savitsky, P, Keates, T, Filippakopoulos, P, Vollmar, M, Yue, W.W, Krojer, T, Ugochukwu, E, von Delft, F, Knapp, S, Weigelt, J, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A.N. | | Deposit date: | 2013-01-23 | | Release date: | 2013-01-30 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (2.58 Å) | | Cite: | Molecular Architecture of the Ankyrin Socs Box Family of Cul5-Dependent E3 Ubiquitin Ligases
J.Mol.Biol., 425, 2013
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3ZTD
 | | pVHL54-213-EloB-EloC complex _ methyl 4-(((2S,4R)-4-hydroxy-1-(2-(3- methylisoxazol-5-yl)acetyl)pyrrolidine-2-carboxamido)methyl)benzoate | | Descriptor: | METHYL 4-[({(4R)-4-HYDROXY-1-[(3-METHYLISOXAZOL-5-YL)ACETYL]-L-PROLYL}AMINO)METHYL]BENZOATE, TRANSCRIPTION ELONGATION FACTOR B POLYPEPTIDE 1, TRANSCRIPTION ELONGATION FACTOR B POLYPEPTIDE 2, ... | | Authors: | VanMolle, I, Buckley, D.L, Crews, C.M, Ciulli, A. | | Deposit date: | 2011-07-07 | | Release date: | 2012-07-25 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.79 Å) | | Cite: | Dissecting Fragment-Based Lead Discovery at the Von Hippel-Lindau Protein:Hypoxia Inducible Factor 1Alpha Protein-Protein Interface.
Chem.Biol., 19, 2012
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3ZTC
 | | pVHL54-213-EloB-EloC complex _ (2S,4R)-N-((1,1'-biphenyl)-4-ylmethyl)- 4-hydroxy-1-(2-(3-methylisoxazol-5-yl)acetyl)pyrrolidine-2- carboxamide | | Descriptor: | (4R)-N-(BIPHENYL-4-YLMETHYL)-4-HYDROXY-1-[(3-METHYLISOXAZOL-5-YL)ACETYL]-L-PROLINAMIDE, TRANSCRIPTION ELONGATION FACTOR B POLYPEPTIDE 1, TRANSCRIPTION ELONGATION FACTOR B POLYPEPTIDE 2, ... | | Authors: | Van Molle, I, Buckley, D.L, Crews, C.M, Ciulli, A. | | Deposit date: | 2011-07-06 | | Release date: | 2012-07-25 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.65 Å) | | Cite: | Dissecting Fragment-Based Lead Discovery at the Von Hippel-Lindau Protein:Hypoxia Inducible Factor 1Alpha Protein-Protein Interface.
Chem.Biol., 19, 2012
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3ZNH
 | | Crimean Congo Hemorrhagic Fever Virus OTU domain in complex with ubiquitin-propargyl. | | Descriptor: | POLYUBIQUITIN-B, UBIQUITIN THIOESTERASE | | Authors: | Ekkebus, R, vanKasteren, S.I, Kulathu, Y, Scholten, A, Berlin, I, deJong, A, Goerdayal, G, Neefjes, J, Heck, A.J.R, Komander, D, Ovaa, H. | | Deposit date: | 2013-02-14 | | Release date: | 2013-02-27 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | On Terminal Alkynes that Can React with Active-Site Cysteine Nucleophiles in Proteases.
J.Am.Chem.Soc., 135, 2013
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3ZNG
 | | Ankyrin repeat and SOCS-box protein 9 (ASB9) in complex with ElonginB and ElonginC | | Descriptor: | 1,2-ETHANEDIOL, ANKYRIN REPEAT AND SOCS BOX PROTEIN 9, TRANSCRIPTION ELONGATION FACTOR B POLYPEPTIDE 1, ... | | Authors: | Thomas, J, Van Molle, I, Ciulli, A. | | Deposit date: | 2013-02-14 | | Release date: | 2013-12-04 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.85 Å) | | Cite: | Multimeric Complexes Among Ankyrin-Repeat and Socs-Box Protein 9 (Asb9), Elonginbc, and Cullin 5: Insights Into the Structure and Assembly of Ecs-Type Cullin-Ring E3 Ubiquitin Ligases.
Biochemistry, 52, 2013
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3ZNZ
 | | Crystal structure of OTULIN OTU domain (C129A) in complex with Met1- di ubiquitin | | Descriptor: | POLYUBIQUITIN-C, PROTEIN FAM105B, SULFATE ION | | Authors: | Keusekotten, K, Elliott, P.R, Glockner, L, Kulathu, Y, Wauer, T, Krappmann, D, Hofmann, K, Komander, D. | | Deposit date: | 2013-02-18 | | Release date: | 2013-06-26 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Otulin Antagonizes Lubac Signaling by Specifically Hydrolyzing met1-Linked Polyubiquitin.
Cell(Cambridge,Mass.), 153, 2013
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8WQE
 | | Cryo-EM structure of CUL2-RBX1-ELOB-ELOC-FEM1B bound with the C-degron of CUX1 (conformation 1) | | Descriptor: | Cullin-2, E3 ubiquitin-protein ligase RBX1, N-terminally processed, ... | | Authors: | Chen, X, Zhang, K, Xu, C. | | Deposit date: | 2023-10-11 | | Release date: | 2024-04-03 | | Last modified: | 2024-05-08 | | Method: | ELECTRON MICROSCOPY (3.38 Å) | | Cite: | Mechanism of Psi-Pro/C-degron recognition by the CRL2 FEM1B ubiquitin ligase.
Nat Commun, 15, 2024
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8WQF
 | | cryo-EM structure of CUL2-RBX1-ELOB-ELOC-FEM1B bound with the C-degron of CUX1 (conformation 2) | | Descriptor: | Cullin-2, E3 ubiquitin-protein ligase RBX1, N-terminally processed, ... | | Authors: | Chen, X, Zhang, K, Xu, C. | | Deposit date: | 2023-10-11 | | Release date: | 2024-04-03 | | Last modified: | 2024-05-08 | | Method: | ELECTRON MICROSCOPY (3.27 Å) | | Cite: | Mechanism of Psi-Pro/C-degron recognition by the CRL2 FEM1B ubiquitin ligase.
Nat Commun, 15, 2024
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8WQC
 | | cryo-EM structure of neddylated CUL2-RBX1-ELOB-ELOC-FEM1B bound with the C-degron of CDK5R1 | | Descriptor: | Cullin-2, E3 ubiquitin-protein ligase RBX1, N-terminally processed, ... | | Authors: | Chen, X, Zhang, K, Xu, C. | | Deposit date: | 2023-10-11 | | Release date: | 2024-04-03 | | Last modified: | 2024-05-08 | | Method: | ELECTRON MICROSCOPY (3.54 Å) | | Cite: | Mechanism of Psi-Pro/C-degron recognition by the CRL2 FEM1B ubiquitin ligase.
Nat Commun, 15, 2024
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8WQG
 | | cryo-EM structure of neddylated CUL2-RBX1-ELOB-ELOC-FEM1B bound with the C-degron of CCDC89 (conformation 1) | | Descriptor: | Cullin-2, E3 ubiquitin-protein ligase RBX1, N-terminally processed, ... | | Authors: | Chen, X, Zhang, K, Xu, C. | | Deposit date: | 2023-10-11 | | Release date: | 2024-04-03 | | Last modified: | 2024-05-08 | | Method: | ELECTRON MICROSCOPY (4.09 Å) | | Cite: | Mechanism of Psi-Pro/C-degron recognition by the CRL2 FEM1B ubiquitin ligase.
Nat Commun, 15, 2024
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8WQA
 | | Cryo-EM structure of CUL2-RBX1-ELOB-ELOC-FEM1B bound with the C-degron of CCDC89 (conformation 1) | | Descriptor: | Coiled-coil domain-containing protein 89, Cullin-2, E3 ubiquitin-protein ligase RBX1, ... | | Authors: | Chen, X, Zhang, K, Xu, C. | | Deposit date: | 2023-10-11 | | Release date: | 2024-04-03 | | Last modified: | 2024-05-08 | | Method: | ELECTRON MICROSCOPY (3.39 Å) | | Cite: | Mechanism of Psi-Pro/C-degron recognition by the CRL2 FEM1B ubiquitin ligase.
Nat Commun, 15, 2024
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8WQH
 | | cryo-EM structure of neddylated CUL2-RBX1-ELOB-ELOC-FEM1B bound with the C-degron of CCDC89 (conformation 2) | | Descriptor: | Coiled-coil domain-containing protein 89, Cullin-2, E3 ubiquitin-protein ligase RBX1, ... | | Authors: | Chen, X, Zhang, K, Xu, C. | | Deposit date: | 2023-10-11 | | Release date: | 2024-04-03 | | Last modified: | 2024-05-08 | | Method: | ELECTRON MICROSCOPY (3.44 Å) | | Cite: | Mechanism of Psi-Pro/C-degron recognition by the CRL2 FEM1B ubiquitin ligase.
Nat Commun, 15, 2024
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8WQB
 | | Cryo-EM structure of CUL2-RBX1-ELOB-ELOC-FEM1B bound with the C-degron of CCDC89 (conformation 2) | | Descriptor: | Coiled-coil domain-containing protein 89, Cullin-2, E3 ubiquitin-protein ligase RBX1, ... | | Authors: | Chen, X, Zhang, K, Xu, C. | | Deposit date: | 2023-10-11 | | Release date: | 2024-04-03 | | Last modified: | 2024-05-08 | | Method: | ELECTRON MICROSCOPY (3.37 Å) | | Cite: | Mechanism of Psi-Pro/C-degron recognition by the CRL2 FEM1B ubiquitin ligase.
Nat Commun, 15, 2024
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9BOL
 | | Crystal structure of the complex between VHL, ElonginB, ElonginC, and compound 5 | | Descriptor: | (4R)-1-[(2S)-2-(4-cyclopropyl-1H-1,2,3-triazol-1-yl)-3,3-dimethylbutanoyl]-4-hydroxy-N-{[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}-L-prolinamide, 1,2-ETHANEDIOL, CHLORIDE ION, ... | | Authors: | Murray, J.M, Wu, H, Fuhrmann, J, Fairbrother, W.J, DiPasquale, A. | | Deposit date: | 2024-05-03 | | Release date: | 2024-05-29 | | Method: | X-RAY DIFFRACTION (1.99 Å) | | Cite: | Potency-enhanced peptidomimetic VHL ligands with improved oral bioavailability
To Be Published
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7JTP
 | | Crystal structure of Protac MS67 in complex with the WD repeat-containing protein 5 and pVHL:ElonginC:ElonginB | | Descriptor: | Elongin-B, Elongin-C, GLYCEROL, ... | | Authors: | Kottur, J, Jain, R, Aggarwal, A.K. | | Deposit date: | 2020-08-18 | | Release date: | 2021-10-06 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.12 Å) | | Cite: | A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models.
Sci Transl Med, 13, 2021
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7JTO
 | | Crystal structure of Protac MS33 in complex with the WD repeat-containing protein 5 and pVHL:ElonginC:ElonginB | | Descriptor: | 1,2-ETHANEDIOL, 3-methyl-N-(11-{[2-(4-{[4'-(4-methylpiperazin-1-yl)-3'-{[6-oxo-4-(trifluoromethyl)-5,6-dihydropyridine-3-carbonyl]amino}[1,1'-biphenyl]-3-yl]methyl}piperazin-1-yl)ethyl]amino}-11-oxoundecanoyl)-L-valyl-(4R)-4-hydroxy-N-{[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}-L-prolinamide, Elongin-B, ... | | Authors: | Kottur, J, Jain, R, Aggarwal, A.K. | | Deposit date: | 2020-08-18 | | Release date: | 2021-10-06 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models.
Sci Transl Med, 13, 2021
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7KHH
 | | Ternary complex of VHL/BRD4-BD1/Compound9 (4-(3,5-difluoropyridin-2-yl)-N-(11-(((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-11-oxoundecyl)-10-methyl-7-((methylsulfonyl)methyl)-11-oxo-3,4,10,11-tetrahydro-1H-1,4,10-triazadibenzo[cd,f]azulene-6-carboxamide) | | Descriptor: | Bromodomain-containing protein 4, Elongin-B, Elongin-C, ... | | Authors: | Murray, J.M. | | Deposit date: | 2020-10-21 | | Release date: | 2021-02-24 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.281 Å) | | Cite: | Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy.
J.Med.Chem., 64, 2021
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7JMS
 | | Structure of the Hazara virus OTU bound to ubiquitin | | Descriptor: | CALCIUM ION, GLYCEROL, Polyubiquitin-B, ... | | Authors: | Dzimianski, J.V, Pegan, S.D. | | Deposit date: | 2020-08-02 | | Release date: | 2020-10-21 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.78 Å) | | Cite: | Flipping the substrate preference of Hazara virus ovarian tumour domain protease through structure-based mutagenesis.
Acta Crystallogr D Struct Biol, 76, 2020
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7JXV
 | | ANTH domain of CALM (clathrin-assembly lymphoid myeloid leukemia protein) bound to ubiquitin | | Descriptor: | Phosphatidylinositol-binding clathrin assembly protein, Ubiquitin | | Authors: | Pashkova, N, Gakhar, L, Schnicker, N.J, Piper, R.C. | | Deposit date: | 2020-08-28 | | Release date: | 2021-08-04 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.35 Å) | | Cite: | ANTH domains within CALM, HIP1R, and Sla2 recognize ubiquitin internalization signals.
Elife, 10, 2021
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4W9H
 | | pVHL:EloB:EloC in complex with (2S,4R)-1-((S)-2-acetamido-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (ligand 7) | | Descriptor: | N-acetyl-3-methyl-L-valyl-(4R)-4-hydroxy-N-[4-(4-methyl-1,3-thiazol-5-yl)benzyl]-L-prolinamide, Transcription elongation factor B polypeptide 1, Transcription elongation factor B polypeptide 2, ... | | Authors: | Gadd, M.S, Soares, P, Galdeano, C, van Molle, I, Ciulli, A. | | Deposit date: | 2014-08-27 | | Release date: | 2014-09-10 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Structure-Guided Design and Optimization of Small Molecules Targeting the Protein-Protein Interaction between the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities.
J.Med.Chem., 57, 2014
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4W9E
 | | pVHL:EloB:EloC in complex with (2S,4R)-1-(3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(thiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (ligand 4) | | Descriptor: | (4R)-1-(3,3-dimethylbutanoyl)-4-hydroxy-N-[4-(1,3-thiazol-5-yl)benzyl]-L-prolinamide, Transcription elongation factor B polypeptide 1, Transcription elongation factor B polypeptide 2, ... | | Authors: | Gadd, M.S, Soares, P, Galdeano, C, van Molle, I, Ciulli, A. | | Deposit date: | 2014-08-27 | | Release date: | 2014-09-10 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Structure-Guided Design and Optimization of Small Molecules Targeting the Protein-Protein Interaction between the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities.
J.Med.Chem., 57, 2014
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4W9F
 | | pVHL:EloB:EloC in complex with (2S,4R)-1-(3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (ligand 5) | | Descriptor: | (4R)-1-(3,3-dimethylbutanoyl)-4-hydroxy-N-[4-(4-methyl-1,3-thiazol-5-yl)benzyl]-L-prolinamide, Transcription elongation factor B polypeptide 1, Transcription elongation factor B polypeptide 2, ... | | Authors: | van Molle, I, Hewitt, S, Galdeano, C, Gadd, M.S, Ciulli, A. | | Deposit date: | 2014-08-27 | | Release date: | 2014-09-10 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Structure-Guided Design and Optimization of Small Molecules Targeting the Protein-Protein Interaction between the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities.
J.Med.Chem., 57, 2014
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4W9J
 | | pVHL:EloB:EloC in complex with (2S,4R)-1-((S)-2-((S)-2-acetamido-4-methylpentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (ligand 13) | | Descriptor: | N-acetyl-L-leucyl-3-methyl-L-valyl-(4R)-4-hydroxy-N-[4-(4-methyl-1,3-thiazol-5-yl)benzyl]-L-prolinamide, Transcription elongation factor B polypeptide 1, Transcription elongation factor B polypeptide 2, ... | | Authors: | Gadd, M.S, Galdeano, C, van Molle, I, Ciulli, A. | | Deposit date: | 2014-08-27 | | Release date: | 2014-09-10 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Structure-Guided Design and Optimization of Small Molecules Targeting the Protein-Protein Interaction between the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities.
J.Med.Chem., 57, 2014
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4W9L
 | | pVHL:EloB:EloC in complex with (2S,4R)-1-((S)-2-((S)-2-acetamido-3,3-dimethylbutanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (ligand 15) | | Descriptor: | N-acetyl-3-methyl-L-valyl-3-methyl-L-valyl-(4R)-4-hydroxy-N-[4-(4-methyl-1,3-thiazol-5-yl)benzyl]-L-prolinamide, Transcription elongation factor B polypeptide 1, Transcription elongation factor B polypeptide 2, ... | | Authors: | Gadd, M.S, Galdeano, C, van Molle, I, Ciulli, A. | | Deposit date: | 2014-08-27 | | Release date: | 2014-09-10 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Structure-Guided Design and Optimization of Small Molecules Targeting the Protein-Protein Interaction between the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities.
J.Med.Chem., 57, 2014
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