7Z77
 
 | | Crystal structure of compound 6 in complex with the bromodomain of human SMARCA2 and pVHL:ElonginC:ElonginB | | 分子名称: | (2~{S},4~{R})-~{N}-[(1~{S})-4-[4-(4-bromanyl-7-cyclopentyl-5-oxidanylidene-benzimidazolo[1,2-a]quinazolin-9-yl)piperidin-1-yl]-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]butyl]-1-[(2~{S})-2-[(1-fluoranylcyclopropyl)carbonylamino]-3,3-dimethyl-butanoyl]-4-oxidanyl-pyrrolidine-2-carboxamide, Elongin-B, Elongin-C, ... | | 著者 | Bader, G, Boettcher, J, Wolkerstorfer, B. | | 登録日 | 2022-03-15 | | 公開日 | 2022-09-14 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (1.97 Å) | | 主引用文献 | A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo.
Nat Commun, 13, 2022
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7S4E
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7Z6L
 | | Crystal structure of PROTAC 5 in complex with the bromodomain of human SMARCA2 and pVHL:ElonginC:ElonginB | | 分子名称: | (2~{S},4~{R})-~{N}-[[2-[3-[4-(4-bromanyl-7-cyclopentyl-5-oxidanylidene-benzimidazolo[1,2-a]quinazolin-9-yl)piperidin-1-yl]propoxy]-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, ... | | 著者 | Roy, M.J, Bader, G, Farnaby, W, Ciulli, A. | | 登録日 | 2022-03-12 | | 公開日 | 2022-09-07 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (2.24 Å) | | 主引用文献 | A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo.
Nat Commun, 13, 2022
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7ZF1
 | | Structure of ubiquitinated FANCI in complex with FANCD2 and double-stranded DNA | | 分子名称: | DNA (61-MER), Fanconi anemia group D2 protein, Fanconi anemia group I protein, ... | | 著者 | Lemonidis, K, Rennie, M.L, Arkinson, C, Streetley, J, Clarke, M, Chaugule, V.K, Walden, H. | | 登録日 | 2022-03-31 | | 公開日 | 2022-11-16 | | 最終更新日 | 2023-02-08 | | 実験手法 | ELECTRON MICROSCOPY (4.14 Å) | | 主引用文献 | Structural and biochemical basis of interdependent FANCI-FANCD2 ubiquitination.
Embo J., 42, 2023
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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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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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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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5TL6
 | | Crystal structure of SARS-CoV papain-like protease in complex with the C-terminal domain of human ISG15 | | 分子名称: | Replicase polyprotein 1ab, SULFATE ION, Ubiquitin-like protein ISG15, ... | | 著者 | Dzimianski, J.V, Daczkowski, C.M, Pegan, S.D. | | 登録日 | 2016-10-10 | | 公開日 | 2017-05-03 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.618 Å) | | 主引用文献 | Structural Insights into the Interaction of Coronavirus Papain-Like Proteases and Interferon-Stimulated Gene Product 15 from Different Species.
J. Mol. Biol., 429, 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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2RR9
 | | The solution structure of the K63-Ub2:tUIMs complex | | 分子名称: | Putative uncharacterized protein UIMC1, ubiquitin | | 著者 | Sekiyama, N, Jee, J, Isogai, S, Akagi, K, Huang, T, Ariyoshi, M, Tochio, H, Shirakawa, M. | | 登録日 | 2010-06-16 | | 公開日 | 2011-07-06 | | 最終更新日 | 2011-07-13 | | 実験手法 | SOLUTION NMR | | 主引用文献 | The solution structure of the K63-Ub2:tUIMs complex
To be Published
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2WDT
 | | Crystal structure of Plasmodium falciparum UCHL3 in complex with the suicide inhibitor UbVME | | 分子名称: | CHLORIDE ION, UBIQUITIN, UBIQUITIN CARBOXYL-TERMINAL HYDROLASE L3 | | 著者 | Weihofen, W.A, Artavanis-Tsakonas, K, Gaudet, R, Ploegh, H.L. | | 登録日 | 2009-03-26 | | 公開日 | 2009-12-29 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Characterization and Structural Studies of the Plasmodium Falciparum Ubiquitin and Nedd8 Hydrolase Uchl3.
J.Biol.Chem., 285, 2010
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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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6R7N
 | | 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 | 2019-03-29 | | 公開日 | 2019-08-28 | | 最終更新日 | 2024-05-22 | | 実験手法 | ELECTRON MICROSCOPY (6.5 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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6R7H
 | | 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, 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 (8.8 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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6R7I
 | | 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.F, Lau, A.M.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 | 2019-09-04 | | 実験手法 | ELECTRON MICROSCOPY (5.9 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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4UEL
 | | UCH-L5 in complex with ubiquitin-propargyl bound to the RPN13 DEUBAD domain | | 分子名称: | POLYUBIQUITIN-B, PROTEASOMAL UBIQUITIN RECEPTOR ADRM1, UBIQUITIN CARBOXYL-TERMINAL HYDROLASE ISOZYME L5 | | 著者 | Sahtoe, D.D, Van Dijk, W.J, El Oualid, F, Ekkebus, R, Ovaa, H, Sixma, T.K. | | 登録日 | 2014-12-18 | | 公開日 | 2015-03-04 | | 最終更新日 | 2019-04-03 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Mechanism of Uch-L5 Activation and Inhibition by Deubad Domains in Rpn13 and Ino80G.
Mol.Cell, 57, 2015
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4UF6
 | | UCH-L5 in complex with ubiquitin-propargyl bound to an activating fragment of INO80G | | 分子名称: | NUCLEAR FACTOR RELATED TO KAPPA-B-BINDING PROTEIN, POLYUBIQUITIN-B, UBIQUITIN CARBOXYL-TERMINAL HYDROLASE ISOZYME L5 | | 著者 | Sahtoe, D.D, Van Dijk, W.J, El Oualid, F, Ekkebus, R, Ovaa, H, Sixma, T.K. | | 登録日 | 2014-12-23 | | 公開日 | 2015-03-04 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (3.69 Å) | | 主引用文献 | Mechanism of Uch-L5 Activation and Inhibition by Deubad Domains in Rpn13 and Ino80G.
Mol.Cell, 57, 2015
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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) | | 分子名称: | (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, ... | | 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 (2.7 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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4W9K
 | | pVHL:EloB:EloC in complex with (2S,4R)-1-((S)-2-((S)-2-acetamido-3-phenylpropanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (ligand 14) | | 分子名称: | N-acetyl-L-phenylalanyl-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, 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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4W9I
 | | pVHL:EloB:EloC in complex with (2S,4R)-1-((2S,4R)-1-acetyl-4-hydroxypyrrolidine-2-carbonyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (ligand 10) | | 分子名称: | (4R)-1-acetyl-4-hydroxy-L-prolyl-(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 (2.4 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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3DBL
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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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