1HV2
 
 | | SOLUTION STRUCTURE OF YEAST ELONGIN C IN COMPLEX WITH A VON HIPPEL-LINDAU PEPTIDE | | 分子名称: | ELONGIN C, VON HIPPEL-LINDAU DISEASE TUMOR SUPPRESSOR | | 著者 | Botuyan, M.V, Mer, G, Yi, G.-S, Koth, C.M, Case, D.A, Edwards, A.M, Chazin, W.J, Arrowsmith, C.H. | | 登録日 | 2001-01-05 | | 公開日 | 2001-09-06 | | 最終更新日 | 2024-05-22 | | 実験手法 | SOLUTION NMR | | 主引用文献 | Solution structure and dynamics of yeast elongin C in complex with a von Hippel-Lindau peptide.
J.Mol.Biol., 312, 2001
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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 | | 分子名称: | 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, ... | | 著者 | VanMolle, I, Buckley, D.L, Crews, C.M, Ciulli, A. | | 登録日 | 2011-07-07 | | 公開日 | 2012-07-25 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (2.79 Å) | | 主引用文献 | 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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1LQB
 | | Crystal structure of a hydroxylated HIF-1 alpha peptide bound to the pVHL/elongin-C/elongin-B complex | | 分子名称: | Elongin B, Elongin C, Hypoxia-inducible factor 1 ALPHA, ... | | 著者 | Hon, W.C, Wilson, M.I, Harlos, K, Claridge, T.D, Schofield, C.J, Pugh, C.W, Maxwell, P.H, Ratcliffe, P.J, Stuart, D.I, Jones, E.Y. | | 登録日 | 2002-05-09 | | 公開日 | 2002-07-03 | | 最終更新日 | 2023-08-16 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Structural basis for the recognition of hydroxyproline in HIF-1 alpha by pVHL.
Nature, 417, 2002
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7S4E
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7CJB
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6SIS
 | | Crystal structure of macrocyclic PROTAC 1 in complex with the second bromodomain of human Brd4 and pVHL:ElonginC:ElonginB | | 分子名称: | Bromodomain-containing protein 4, Elongin-B, Elongin-C, ... | | 著者 | Hughes, S.J, Testa, A, Ciulli, A. | | 登録日 | 2019-08-10 | | 公開日 | 2019-12-04 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (3.5 Å) | | 主引用文献 | Structure-Based Design of a Macrocyclic PROTAC.
Angew.Chem.Int.Ed.Engl., 59, 2020
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6ZHC
 | | PROTAC6 mediated complex of VHL:EloB:EloC and Bcl-xL | | 分子名称: | 1,2-ETHANEDIOL, 2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1~{H}-isoquinolin-2-yl]-5-[3-[4-[3-[2-[2-[2-[2-[2-[3-[[(2~{S})-3,3-dimethyl-1-[(2~{S},4~{R})-2-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methylcarbamoyl]-4-oxidanyl-pyrrolidin-1-yl]-1-oxidanylidene-butan-2-yl]amino]-3-oxidanylidene-propoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]prop-1-ynyl]phenoxy]propyl]-1,3-thiazole-4-carboxylic acid, Bcl-2-like protein 1, ... | | 著者 | Chung, C. | | 登録日 | 2020-06-22 | | 公開日 | 2020-08-05 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (1.92 Å) | | 主引用文献 | Structural Insights into PROTAC-Mediated Degradation of Bcl-xL.
Acs Chem.Biol., 15, 2020
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5LLI
 | | pVHL:EloB:EloC in complex with VH298 | | 分子名称: | (2~{S},4~{R})-1-[(2~{S})-2-[(1-cyanocyclopropyl)carbonylamino]-3,3-dimethyl-butanoyl]-~{N}-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]-4-oxidanyl-pyrrolidine-2-carboxamide, Transcription elongation factor B polypeptide 1, Transcription elongation factor B polypeptide 2, ... | | 著者 | Gadd, M.S, Soares, P, Galdeano, C, Ciulli, A. | | 登録日 | 2016-07-27 | | 公開日 | 2016-11-09 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Potent and selective chemical probe of hypoxic signalling downstream of HIF-alpha hydroxylation via VHL inhibition.
Nat Commun, 7, 2016
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6BVB
 | | Crystal structure of HIF-2alpha-pVHL-elongin B-elongin C | | 分子名称: | Elongin-B, Elongin-C, Hypoxia-Inducible Factor 2 alpha, ... | | 著者 | Tarade, D, Ohh, M, Lee, J.E. | | 登録日 | 2017-12-12 | | 公開日 | 2018-08-01 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.002 Å) | | 主引用文献 | HIF-2 alpha-pVHL complex reveals broad genotype-phenotype correlations in HIF-2 alpha-driven disease.
Nat Commun, 9, 2018
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1VCB
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5T35
 | | The PROTAC MZ1 in complex with the second bromodomain of Brd4 and pVHL:ElonginC:ElonginB | | 分子名称: | (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, ... | | 著者 | Gadd, M.S, Zengerle, M, Ciulli, A. | | 登録日 | 2016-08-24 | | 公開日 | 2017-03-08 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Structural basis of PROTAC cooperative recognition for selective protein degradation.
Nat. Chem. Biol., 13, 2017
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9BOL
 | | Crystal structure of the complex between VHL, ElonginB, ElonginC, and compound 5 | | 分子名称: | (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, ... | | 著者 | Murray, J.M, Wu, H, Fuhrmann, J, Fairbrother, W.J, DiPasquale, A. | | 登録日 | 2024-05-03 | | 公開日 | 2024-05-29 | | 実験手法 | X-RAY DIFFRACTION (1.99 Å) | | 主引用文献 | Potency-enhanced peptidomimetic VHL ligands with improved oral bioavailability
To Be Published
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9BJU
 | | Crystal structure of the complex between VHL, ElonginB, ElonginC, and compound 5 | | 分子名称: | 1,2-ETHANEDIOL, 3-PYRIDIN-4-YL-2,4-DIHYDRO-INDENO[1,2-.C.]PYRAZOLE, ACETATE ION, ... | | 著者 | Murray, J.M, Wu, H, Fuhrmann, J, Fairbrother, W.J, DiPasquale, A. | | 登録日 | 2024-04-25 | | 公開日 | 2024-05-29 | | 実験手法 | X-RAY DIFFRACTION (2.47 Å) | | 主引用文献 | Potency-enhanced peptidomimetic VHL ligands with improved oral bioavailability
To Be Published
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6R7F
 | | Structural basis of Cullin-2 RING E3 ligase regulation by the COP9 signalosome | | 分子名称: | COP9 signalosome complex subunit 1, COP9 signalosome complex subunit 2, COP9 signalosome complex subunit 3, ... | | 著者 | Faull, S.V, Lau, A.M.C, Martens, C, Ahdash, Z, Yebenes, H, Schmidt, C, Beuron, F, Cronin, N.B, Morris, E.P, Politis, A. | | 登録日 | 2019-03-28 | | 公開日 | 2019-08-28 | | 最終更新日 | 2024-05-22 | | 実験手法 | ELECTRON MICROSCOPY (8.2 Å) | | 主引用文献 | Structural basis of Cullin 2 RING E3 ligase regulation by the COP9 signalosome.
Nat Commun, 10, 2019
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6R6H
 | | Structural basis of Cullin-2 RING E3 ligase regulation by the COP9 signalosome | | 分子名称: | COP9 signalosome complex subunit 1, COP9 signalosome complex subunit 2, COP9 signalosome complex subunit 3, ... | | 著者 | Morris, E.P, Faull, S.V, Lau, A.M.C, Politis, A, Beuron, F, Cronin, N. | | 登録日 | 2019-03-27 | | 公開日 | 2019-08-28 | | 最終更新日 | 2024-05-22 | | 実験手法 | ELECTRON MICROSCOPY (8.4 Å) | | 主引用文献 | Structural basis of Cullin 2 RING E3 ligase regulation by the COP9 signalosome.
Nat Commun, 10, 2019
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8VLB
 | | Crystal structure of EloBC-VHL-CDO1 complex bound to compound 4 molecular glue | | 分子名称: | CITRIC ACID, Cysteine dioxygenase type 1, Elongin-B, ... | | 著者 | Shu, W, Ma, X, Tutter, A, Buckley, D, Golosov, A, Michaud, G. | | 登録日 | 2024-01-11 | | 公開日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | A small molecule VHL molecular glue degrader for cysteine dioxygenase 1
To Be Published
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8VL9
 | | Crystal structure of EloBC-VHL-CDO1 complex bound to compound 8 molecular glue | | 分子名称: | CITRIC ACID, Cysteine dioxygenase type 1, Elongin-B, ... | | 著者 | Shu, W, Ma, X, Tutter, A, Buckley, D, Golosov, A, Michaud, G. | | 登録日 | 2024-01-11 | | 公開日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | A small molecule VHL molecular glue degrader for cysteine dioxygenase 1
To Be Published
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7PI4
 | | FAK Protac GSK215 in complex with FAK and pVHL:ElonginC:ElonginB | | 分子名称: | (2S,4R)-4-hydroxy-1-((S)-2-(2-(4-(3-methoxy-4-((4-((2-(methylcarbamoyl)phenyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide, 1,2-ETHANEDIOL, CALCIUM ION, ... | | 著者 | Chung, C. | | 登録日 | 2021-08-19 | | 公開日 | 2021-09-29 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (2.24 Å) | | 主引用文献 | Discovery and Characterisation of Highly Cooperative FAK-Degrading PROTACs.
Angew.Chem.Int.Ed.Engl., 60, 2021
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7Q2J
 | | Quaternary Complex of human WDR5 and pVHL:ElonginC:ElonginB bound to PROTAC Homer | | 分子名称: | Elongin-B, Elongin-C, N-[5-[4-[[5-[[(2S)-3,3-dimethyl-1-[(2S,4R)-2-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methylcarbamoyl]-4-oxidanyl-pyrrolidin-1-yl]-1-oxidanylidene-butan-2-yl]amino]-5-oxidanylidene-pentyl]carbamoyl]phenyl]-2-(4-methylpiperazin-1-yl)phenyl]-6-oxidanylidene-4-(trifluoromethyl)-1H-pyridine-3-carboxamide, ... | | 著者 | Kraemer, A, Doelle, A, Schwalm, M.P, Adhikari, B, Wolf, E, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2021-10-25 | | 公開日 | 2021-11-24 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Tracking the PROTAC degradation pathway in living cells highlights the importance of ternary complex measurement for PROTAC optimization.
Cell Chem Biol, 30, 2023
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8P0F
 | | Crystal structure of the VCB complex with compound 1. | | 分子名称: | (3~{R},5~{R})-~{N}-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]-5-oxidanyl-2-oxidanylidene-1-pyridin-2-yl-piperidine-3-carboxamide, CHLORIDE ION, Elongin-B, ... | | 著者 | Bader, G, Boettcher, J, Wolkerstorfer, B. | | 登録日 | 2023-05-10 | | 公開日 | 2023-05-31 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (1.98 Å) | | 主引用文献 | Drugit: Crowd-sourcing molecular design of non-peptidic VHL binders
Chemrxiv, 2023
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8PC2
 | | SelDeg51 in complex with FKBP51FK1 domain and pVHL:EloB:EloC | | 分子名称: | Elongin-B, Elongin-C, Peptidyl-prolyl cis-trans isomerase FKBP5, ... | | 著者 | Meyners, C, Walz, M, Geiger, T.M, Hausch, F. | | 登録日 | 2023-06-09 | | 公開日 | 2023-11-15 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | 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
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1LM8
 | | Structure of a HIF-1a-pVHL-ElonginB-ElonginC Complex | | 分子名称: | ELONGIN B, ELONGIN C, Hypoxia-inducible factor 1 alpha, ... | | 著者 | Min, J.-H, Yang, H, Ivan, M, Gertler, F, Kaelin JR, W.G, Pavletich, N.P. | | 登録日 | 2002-04-30 | | 公開日 | 2002-06-12 | | 最終更新日 | 2023-08-16 | | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | | 主引用文献 | Structure of an HIF-1alpha -pVHL complex: hydroxyproline recognition in signaling.
Science, 296, 2002
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4W9C
 | | pVHL:EloB:EloC in complex with (2S,4R)-1-(3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(oxazol-5-yl)benzyl)pyrrolidine-2-carboxamide (ligand 2) | | 分子名称: | (4R)-1-(3,3-dimethylbutanoyl)-4-hydroxy-N-[4-(1,3-oxazol-5-yl)benzyl]-L-prolinamide, Transcription elongation factor B polypeptide 1, Transcription elongation factor B polypeptide 2, ... | | 著者 | Gadd, M.S, Hewitt, S, Galdeano, C, van Molle, I, Ciulli, A. | | 登録日 | 2014-08-27 | | 公開日 | 2014-09-10 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | 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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4W9D
 | | pVHL:EloB:EloC in complex with (2S,4R)-1-(3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methyloxazol-5-yl)benzyl)pyrrolidine-2-carboxamide (ligand 3) | | 分子名称: | (4R)-1-(3,3-dimethylbutanoyl)-4-hydroxy-N-[4-(4-methyl-1,3-oxazol-5-yl)benzyl]-L-prolinamide, Transcription elongation factor B polypeptide 1, Transcription elongation factor B polypeptide 2, ... | | 著者 | Gadd, M.S, Hewitt, S, Galdeano, C, van Molle, I, Ciulli, A. | | 登録日 | 2014-08-27 | | 公開日 | 2014-09-10 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | 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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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) | | 分子名称: | 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, ... | | 著者 | Gadd, M.S, Soares, P, Galdeano, C, van Molle, I, Ciulli, A. | | 登録日 | 2014-08-27 | | 公開日 | 2014-09-10 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | 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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