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
|
|
7ZLN
 | | Crystal structure of SOCS2:ElonginB:ElonginC in complex with compound 11 | | Descriptor: | Elongin-B, Elongin-C, Suppressor of cytokine signaling 2, ... | | Authors: | Ramachandran, S, Ciulli, A, Makukhin, N. | | Deposit date: | 2022-04-15 | | Release date: | 2023-04-26 | | Last modified: | 2024-05-01 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2.
Nat Commun, 14, 2023
|
|
8EBN
 | | Structure of KLHDC2-EloB/C tetrameric assembly | | Descriptor: | Elongin-B, Elongin-C, Kelch domain-containing protein 2 | | Authors: | Scott, D.C, Schulman, B.A. | | Deposit date: | 2022-08-31 | | Release date: | 2023-02-22 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | E3 ligase autoinhibition by C-degron mimicry maintains C-degron substrate fidelity.
Mol.Cell, 83, 2023
|
|
8CQK
 | | pVHL:EloB:EloC in complex with (2S,4R)-1-((S)-2-(1-Fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(2-methyl-4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide (Compound 30) | | Descriptor: | (2~{S},4~{R})-1-[(2~{S})-2-[(1-fluoranylcyclopropyl)carbonylamino]-3,3-dimethyl-butanoyl]-~{N}-[(1~{S})-1-[2-methyl-4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]-4-oxidanyl-pyrrolidine-2-carboxamide, Elongin-B, Elongin-C, ... | | Authors: | Casement, R, Phuong Vu, L, Ciulli, A, Gutschow, M. | | Deposit date: | 2023-03-06 | | Release date: | 2023-09-27 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.62 Å) | | Cite: | Expanding the Structural Diversity at the Phenylene Core of Ligands for the von Hippel-Lindau E3 Ubiquitin Ligase: Development of Highly Potent Hypoxia-Inducible Factor-1 alpha Stabilizers.
J.Med.Chem., 66, 2023
|
|
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
|
|
6I4X
 | | Crystal structure of SOCS2:Elongin C:Elongin B in complex with erythropoietin receptor peptide | | Descriptor: | DI(HYDROXYETHYL)ETHER, Elongin-B, Elongin-C, ... | | Authors: | Kung, W.W, Ramachandran, S, Makukhin, N, Bruno, E, Ciulli, A. | | Deposit date: | 2018-11-12 | | Release date: | 2019-05-29 | | Last modified: | 2019-06-19 | | Method: | X-RAY DIFFRACTION (2.69 Å) | | Cite: | Structural insights into substrate recognition by the SOCS2 E3 ubiquitin ligase.
Nat Commun, 10, 2019
|
|
4W9G
 | | pVHL:EloB:EloC in complex with (2S,4R)-1-(3,3-dimethylbutanoyl)-4-hydroxy-N-(3-methyl-4-(thiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (ligand 6) | | Descriptor: | (4R)-1-(3,3-dimethylbutanoyl)-4-hydroxy-N-[3-methyl-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 (2.7 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
|
|
8CX0
 | | Cryo-EM structure of human APOBEC3G/HIV-1 Vif/CBFbeta/ELOB/ELOC monomeric complex | | Descriptor: | Core-binding factor subunit beta, DNA dC->dU-editing enzyme APOBEC-3G, Elongin-B, ... | | Authors: | Li, Y, Langley, C, Azumaya, C.M, Echeverria, I, Chesarino, N.M, Emerman, M, Cheng, Y, Gross, J.D. | | Deposit date: | 2022-05-19 | | Release date: | 2023-02-15 | | Last modified: | 2024-06-12 | | Method: | ELECTRON MICROSCOPY (2.7 Å) | | Cite: | The structural basis for HIV-1 Vif antagonism of human APOBEC3G.
Nature, 615, 2023
|
|
5NVZ
 | | pVHL:EloB:EloC in complex with (2S,4R)-1-((S)-2-(1-acetylcyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (ligand 16) | | Descriptor: | (2~{S},4~{R})-1-[(2~{S})-2-[(1-ethanoylcyclopropyl)carbonylamino]-3,3-dimethyl-butanoyl]-~{N}-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]-4-oxidanyl-pyrrolidine-2-carboxamide, Elongin-B, Elongin-C, ... | | Authors: | Gadd, M.S, Soares, P, Ciulli, A. | | Deposit date: | 2017-05-04 | | Release date: | 2017-09-20 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase: Structure-Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298).
J. Med. Chem., 61, 2018
|
|
6GFY
 | | pVHL:EloB:EloC in complex with modified VH032 containing (3R,4S)-3-fluoro-4-hydroxyproline (ligand 14a) | | Descriptor: | (2~{R},3~{R},4~{S})-1-[(2~{S})-2-acetamido-3,3-dimethyl-butanoyl]-3-fluoranyl-~{N}-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]-4-oxidanyl-pyrrolidine-2-carboxamide, Elongin-B, Elongin-C, ... | | Authors: | Gadd, M.S, Testa, A, Ciulli, A. | | Deposit date: | 2018-05-02 | | Release date: | 2018-07-11 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | 3-Fluoro-4-hydroxyprolines: Synthesis, Conformational Analysis, and Stereoselective Recognition by the VHL E3 Ubiquitin Ligase for Targeted Protein Degradation.
J. Am. Chem. Soc., 140, 2018
|
|
8BDT
 | | Ternary complex between VCB, BRD4-BD2 and PROTAC 51 | | Descriptor: | (2~{S},4~{R})-~{N}-[(1~{S})-3-[2-[2-[2-[2-[2-[(9~{S})-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.0^{2,6}]trideca-2(6),4,7,10,12-pentaen-9-yl]ethanoylamino]ethoxy]ethoxy]ethoxy]ethylamino]-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]-3-oxidanylidene-propyl]-1-[(2~{R})-3-methyl-2-(3-methyl-1,2-oxazol-5-yl)butanoyl]-4-oxidanyl-pyrrolidine-2-carboxamide, Bromodomain-containing protein 4, Elongin-B, ... | | Authors: | Sorrell, F.J, Mueller, J.E, Lehmann, M, Wegener, A.A. | | Deposit date: | 2022-10-20 | | Release date: | 2023-02-15 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Systematic Potency and Property Assessment of VHL Ligands and Implications on PROTAC Design.
Chemmedchem, 18, 2023
|
|
8G1P
 | | Co-crystal structure of Compound 11 in complex with the bromodomain of human SMARCA2 and pVHL:ElonginC:ElonginB | | Descriptor: | (2~{S},4~{R})-~{N}-[[2-[2-[4-[[4-[3-azanyl-6-(2-hydroxyphenyl)pyridazin-4-yl]piperazin-1-yl]methyl]phenyl]ethoxy]-4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]-1-[(2~{S})-2-[(1-fluoranylcyclopropyl)carbonylamino]-3,3-dimethyl-butanoyl]-4-oxidanyl-pyrrolidine-2-carboxamide, Elongin-B, Elongin-C, ... | | Authors: | Ghimire Rijal, S, Wurz, R.P, Vaish, A. | | Deposit date: | 2023-02-02 | | Release date: | 2023-07-26 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Affinity and cooperativity modulate ternary complex formation to drive targeted protein degradation.
Nat Commun, 14, 2023
|
|
5T35
 | | The PROTAC MZ1 in complex with the second bromodomain of Brd4 and pVHL:ElonginC:ElonginB | | Descriptor: | (2~{S},4~{R})-1-[(2~{S})-2-[2-[2-[2-[2-[2-[(9~{S})-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.0^{2,6}]trideca-2(6),4,7,10,12-pentaen-9-yl]ethanoylamino]ethoxy]ethoxy]ethoxy]ethanoylamino]-3,3-dimethyl-butanoyl]-~{N}-[[4-(4-methyl-2,3-dihydro-1,3-thiazol-5-yl)phenyl]methyl]-4-oxidanyl-pyrrolidine-2-carboxamide, Bromodomain-containing protein 4, Transcription elongation factor B polypeptide 1, ... | | Authors: | Gadd, M.S, Zengerle, M, Ciulli, A. | | Deposit date: | 2016-08-24 | | Release date: | 2017-03-08 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Structural basis of PROTAC cooperative recognition for selective protein degradation.
Nat. Chem. Biol., 13, 2017
|
|
1VCB
 | | THE VHL-ELONGINC-ELONGINB STRUCTURE | | Descriptor: | PROTEIN (ELONGIN B), PROTEIN (ELONGIN C), PROTEIN (VHL) | | Authors: | Stebbins, C.E, Kaelin, W.G, Pavletich, N.P. | | Deposit date: | 1999-03-13 | | Release date: | 1999-04-21 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Structure of the VHL-ElonginC-ElonginB complex: implications for VHL tumor suppressor function.
Science, 284, 1999
|
|
6FMK
 | | pVHL:EloB:EloC in complex with N-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamothioyl) pyrrolidin-1-yl)-1-thioxopropan-2-yl)acetamide (ligand 4) | | Descriptor: | Elongin-B, Elongin-C, von Hippel-Lindau disease tumor suppressor, ... | | Authors: | Soares, P, Lucas, X, Ciulli, A. | | Deposit date: | 2018-01-31 | | Release date: | 2018-04-11 | | Last modified: | 2018-06-20 | | Method: | X-RAY DIFFRACTION (2.75 Å) | | Cite: | Thioamide substitution to probe the hydroxyproline recognition of VHL ligands.
Bioorg. Med. Chem., 26, 2018
|
|
6GMQ
 | | pVHL:EloB:EloC in complex with (4-(1H-pyrrol-1-yl)phenyl)methanol | | Descriptor: | (4-pyrrol-1-ylphenyl)methanol, ACETATE ION, Elongin-B, ... | | Authors: | Van Molle, I, Lucas, X, Ciulli, A. | | Deposit date: | 2018-05-28 | | Release date: | 2018-08-22 | | Last modified: | 2018-09-05 | | Method: | X-RAY DIFFRACTION (2.755 Å) | | Cite: | Surface Probing by Fragment-Based Screening and Computational Methods Identifies Ligandable Pockets on the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase.
J. Med. Chem., 61, 2018
|
|
8BDN
 | | VCB in complex with compound 23 | | Descriptor: | (2~{R})-3-methyl-1-[(2~{S},4~{R})-2-[(5~{R})-5-methyl-5-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]-4~{H}-1,2,4-oxadiazol-3-yl]-4-oxidanyl-pyrrolidin-1-yl]-2-(3-methyl-1,2-oxazol-5-yl)butan-1-one, Elongin-B, Elongin-C, ... | | Authors: | Sorrell, F.J, Mueller, J.E, Lehmann, M, Wegener, A. | | Deposit date: | 2022-10-19 | | Release date: | 2023-02-15 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.76 Å) | | Cite: | Systematic Potency and Property Assessment of VHL Ligands and Implications on PROTAC Design.
Chemmedchem, 18, 2023
|
|
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
|
|
8OEW
 | | Structure of the mammalian Pol II-Elongin complex, lacking the ELOA latch (composite structure, structure 2) | | Descriptor: | DNA-directed RNA polymerase II subunit E, DNA-directed RNA polymerase II subunit F, DNA-directed RNA polymerase II subunit RPB1, ... | | Authors: | Chen, Y, Kokic, G, Dienemann, C, Dybkov, O, Urlaub, H, Cramer, P. | | Deposit date: | 2023-03-13 | | Release date: | 2023-10-18 | | Last modified: | 2023-12-27 | | Method: | ELECTRON MICROSCOPY (2.8 Å) | | Cite: | Structure of the transcribing RNA polymerase II-Elongin complex.
Nat.Struct.Mol.Biol., 30, 2023
|
|
6I5J
 | | Crystal structure of SOCS2:Elongin C:Elongin B in complex with growth hormone receptor peptide | | Descriptor: | COBALT (II) ION, Elongin-B, Elongin-C, ... | | Authors: | Kung, W.W, Ramachandran, S, Makukhin, N, Bruno, E, Ciulli, A. | | Deposit date: | 2018-11-13 | | Release date: | 2019-05-29 | | Last modified: | 2019-11-20 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Structural insights into substrate recognition by the SOCS2 E3 ubiquitin ligase.
Nat Commun, 10, 2019
|
|
7CJB
 | |
8PC2
 | | SelDeg51 in complex with FKBP51FK1 domain and pVHL:EloB:EloC | | Descriptor: | Elongin-B, Elongin-C, Peptidyl-prolyl cis-trans isomerase FKBP5, ... | | Authors: | Meyners, C, Walz, M, Geiger, T.M, Hausch, F. | | Deposit date: | 2023-06-09 | | Release date: | 2023-11-15 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Discovery of a Potent Proteolysis Targeting Chimera Enables Targeting the Scaffolding Functions of FK506-Binding Protein 51 (FKBP51).
Angew.Chem.Int.Ed.Engl., 63, 2024
|
|
7PLO
 | | H. sapiens replisome-CUL2/LRR1 complex | | Descriptor: | Cell division control protein 45 homolog, Claspin, Cullin-2, ... | | Authors: | Jones, M.J, Yeeles, J.T.P, Deegan, T.D, Jenkyn-Bedford, M. | | Deposit date: | 2021-09-01 | | Release date: | 2021-11-10 | | Last modified: | 2023-10-18 | | Method: | ELECTRON MICROSCOPY (2.8 Å) | | Cite: | A conserved mechanism for regulating replisome disassembly in eukaryotes.
Nature, 600, 2021
|
|
8BB4
 | | Structure of human WDR5 and pVHL:ElonginC:ElonginB bound to PROTAC with C3 linker | | Descriptor: | Elongin-B, Elongin-C, WD repeat-containing protein 5, ... | | Authors: | Kraemer, A, Doelle, A, Knapp, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2022-10-12 | | Release date: | 2022-11-09 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Tracking the PROTAC degradation pathway in living cells highlights the importance of ternary complex measurement for PROTAC optimization.
Cell Chem Biol, 30, 2023
|
|
6FMI
 | | pVHL:EloB:EloC in complex with N-((S)-1-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamothioyl) pyrrolidin-1-yl)-1-oxopropan-2-yl)acetamide (ligand 2) | | Descriptor: | Elongin-B, Elongin-C, von Hippel-Lindau disease tumor suppressor, ... | | Authors: | Soares, P, Lucas, X, Ciulli, A. | | Deposit date: | 2018-01-31 | | Release date: | 2018-04-11 | | Last modified: | 2018-06-20 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Thioamide substitution to probe the hydroxyproline recognition of VHL ligands.
Bioorg. Med. Chem., 26, 2018
|
|
