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PDB: 157 件
8BB3
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Structure of human WDR5 and pVHL:ElonginC:ElonginB bound to PROTAC with PEG linker (conformation #1)
分子名称: 1,2-ETHANEDIOL, Elongin-B, Elongin-C, ...
著者Kraemer, A, Doelle, A, Knapp, S, Structural Genomics Consortium (SGC)
登録日2022-10-12
公開日2022-11-09
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (1.8 Å)
主引用文献Structure of human WDR5 and pVHL:ElonginC:ElonginB bound to PROTAC with PEG linker (conformation #1)
To Be Published
2GNQ
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Structure of wdr5
分子名称: CHLORIDE ION, WD-repeat protein 5
著者Min, J, Schuetz, A, Allali-Hassani, A, Loppnau, P, Vedadi, M, Weigelt, J, Sundstrom, M, Edwards, A.M, Arrowsmith, C.H, Bochkarev, A, Plotnikov, A.N, Structural Genomics Consortium (SGC)
登録日2006-04-10
公開日2006-06-06
最終更新日2023-08-30
実験手法X-RAY DIFFRACTION (1.8 Å)
主引用文献Structural basis for molecular recognition and presentation of histone H3 By WDR5.
Embo J., 25, 2006
7UAS
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Discovery of Potent Orally Bioavailable WD Repeat Domain 5 (WDR5) Inhibitors Using a Pharmacophore-Based Optimization
分子名称: (5P)-2-[(S)-cyclopropyl(4-methylpyridin-2-yl)methyl]-5-[1-ethyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-7-[(2-methyl-1H-imidazol-1-yl)methyl]-3,4-dihydroisoquinolin-1(2H)-one, WD repeat-containing protein 5
著者Zhao, B.
登録日2022-03-14
公開日2022-05-04
最終更新日2023-10-18
実験手法X-RAY DIFFRACTION (1.808 Å)
主引用文献Discovery of Potent Orally Bioavailable WD Repeat Domain 5 (WDR5) Inhibitors Using a Pharmacophore-Based Optimization.
J.Med.Chem., 65, 2022
6PGC
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BU of 6pgc by Molmil
WDR5delta32 bound to methyl benzyl(4-(4-(hydroxymethyl)-1H-imidazol-2-yl)butyl)carbamate
分子名称: SULFATE ION, WD repeat-containing protein 5, methyl benzyl{4-[4-(hydroxymethyl)-1H-imidazol-2-yl]butyl}carbamate
著者Dennis, M.L, Peat, T.S.
登録日2019-06-24
公開日2019-12-11
最終更新日2023-10-11
実験手法X-RAY DIFFRACTION (1.81 Å)
主引用文献Fragment screening for a protein-protein interaction inhibitor to WDR5.
Struct Dyn., 6, 2019
4ES0
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X-ray structure of WDR5-SETd1b Win motif peptide binary complex
分子名称: Histone-lysine N-methyltransferase SETD1B, WD repeat-containing protein 5
著者Dharmarajan, V, Lee, J.-H, Patel, A, Skalnik, D.G, Cosgrove, M.S.
登録日2012-04-21
公開日2012-05-30
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (1.817 Å)
主引用文献Structural basis for WDR5 interaction (Win) motif recognition in human SET1 family histone methyltransferases.
J.Biol.Chem., 287, 2012
3SMR
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BU of 3smr by Molmil
Crystal structure of human WD repeat domain 5 with compound
分子名称: 1,2-ETHANEDIOL, 2-chloro-N-[2-(4-methylpiperazin-1-yl)-5-nitrophenyl]benzamide, UNKNOWN ATOM OR ION, ...
著者Dong, A, Dombrovski, L, Wasney, G.A, Tempel, W, Senisterra, G, Bolshan, Y, Smil, D, Nguyen, K.T, Hajian, T, Poda, G, Al-Awar, R, Bountra, C, Weigelt, J, Edwards, A.M, Brown, P.J, Schapira, M, Arrowsmith, C.H, Vedadi, M, Wu, H, Structural Genomics Consortium (SGC)
登録日2011-06-28
公開日2011-08-31
最終更新日2023-09-13
実験手法X-RAY DIFFRACTION (1.82 Å)
主引用文献Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5.
Biochem. J., 449, 2013
6D9X
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Discovery of Potent 2-Aryl-6,7-Dihydro-5HPyrrolo[ 1,2-a]imidazoles as WDR5 WIN-site Inhibitors Using Fragment-Based Methods and Structure-Based Design
分子名称: 2-phenyl-6,7-dihydro-5H-pyrrolo[1,2-a]imidazole, SODIUM ION, WD repeat-containing protein 5
著者Phan, J, Fesik, S.W.
登録日2018-04-30
公開日2018-09-05
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (1.83 Å)
主引用文献Discovery of Potent 2-Aryl-6,7-dihydro-5 H-pyrrolo[1,2- a]imidazoles as WDR5-WIN-Site Inhibitors Using Fragment-Based Methods and Structure-Based Design.
J. Med. Chem., 61, 2018
8WXT
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Structure of WDR5 in complex with WIN motif containing MBD3C R45E/V46G
分子名称: MBD3C, WD repeat-containing protein 5
著者Xu, L, Yang, Y.
登録日2023-10-30
公開日2024-06-26
実験手法X-RAY DIFFRACTION (1.83 Å)
主引用文献Structural studies of WDR5 in complex with MBD3C WIN motif reveal a unique binding mode.
J.Biol.Chem., 2024
8Q1N
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Cyclic peptide binder of the WBM-site of WDR5
分子名称: Cyclic peptide inhibitor, WD repeat-containing protein 5
著者Schmeing, S, Chang, J.Y, t Hart, P, Gasper, R.
登録日2023-08-01
公開日2023-09-06
最終更新日2023-09-13
実験手法X-RAY DIFFRACTION (1.843 Å)
主引用文献Macrocyclic peptides as inhibitors of WDR5-lncRNA interactions.
Chem.Commun.(Camb.), 59, 2023
6UCS
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Discovery and Structure-Based optimization of potent and selective WDR5 inhibitors containing a dihydroisoquinolinone bicyclic core
分子名称: 2-amino-3-{[(5P)-2-[(3,5-dimethoxyphenyl)methyl]-5-(4-fluoro-2-methylphenyl)-1-oxo-1,2,3,4-tetrahydroisoquinolin-7-yl]methyl}-1-methyl-1H-imidazol-3-ium, WD repeat-containing protein 5
著者Zhao, B.
登録日2019-09-17
公開日2020-01-01
最終更新日2024-05-15
実験手法X-RAY DIFFRACTION (1.85 Å)
主引用文献Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core.
J.Med.Chem., 63, 2020
6OFZ
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Crystal structure of human WDR5
分子名称: WD repeat-containing protein 5
著者Lorton, B.M, Harijan, R.K, Burgos, E, Bonanno, J.B, Almo, S.C, Shechter, D.
登録日2019-04-01
公開日2020-04-01
最終更新日2023-10-11
実験手法X-RAY DIFFRACTION (1.85 Å)
主引用文献A Binary Arginine Methylation Switch on Histone H3 Arginine 2 Regulates Its Interaction with WDR5.
Biochemistry, 59, 2020
8X3S
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Crystal structure of human WDR5 in complex with PTEN
分子名称: Phosphatidylinositol 3,4,5-trisphosphate 3-phosphatase and dual-specificity protein phosphatase PTEN, WD repeat-containing protein 5
著者Liu, Y, Huang, X, Shang, X.
登録日2023-11-14
公開日2024-05-29
実験手法X-RAY DIFFRACTION (1.87 Å)
主引用文献The NTE domain of PTEN alpha / beta promotes cancer progression by interacting with WDR5 via its SSSRRSS motif.
Cell Death Dis, 15, 2024
2H6Q
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Histone H3 recognition and presentation by the WDR5 module of the MLL1 complex
分子名称: Histone H3 K4-Me3 9-residue peptide, WD-repeat protein 5
著者Ruthenburg, A.J, Wang, W.-K, Graybosch, D.M, Li, H, Allis, C.D, Patel, D.J, Verdine, G.L.
登録日2006-06-01
公開日2006-07-04
最終更新日2023-08-30
実験手法X-RAY DIFFRACTION (1.87 Å)
主引用文献Histone H3 recognition and presentation by the WDR5 module of the MLL1 complex.
Nat.Struct.Mol.Biol., 13, 2006
4O45
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WDR5 in complex with influenza NS1 C-terminal tail
分子名称: Nonstructural protein 1, UNKNOWN ATOM OR ION, WD repeat-containing protein 5
著者Qin, S, Xu, C, Tempel, W, Arrowsmith, C.H, Bountra, C, Edwards, A.M, Min, J, Structural Genomics Consortium (SGC)
登録日2013-12-18
公開日2014-04-23
最終更新日2024-04-03
実験手法X-RAY DIFFRACTION (1.87 Å)
主引用文献Structural basis for histone mimicry and hijacking of host proteins by influenza virus protein NS1.
Nat Commun, 5, 2014
6DAR
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BU of 6dar by Molmil
Discovery of Potent 2-Aryl-6,7-Dihydro-5HPyrrolo[ 1,2-a]imidazoles as WDR5 WIN-site Inhibitors Using Fragment-Based Methods and Structure-Based Design
分子名称: DIMETHYL SULFOXIDE, N-(cyclopropylmethyl)-N-{[3-(6,7-dihydro-5H-pyrrolo[1,2-a]imidazol-2-yl)phenyl]methyl}-3-methoxybenzamide, SULFATE ION, ...
著者Phan, J, Fesik, S.W.
登録日2018-05-01
公開日2018-09-05
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (1.88 Å)
主引用文献Discovery of Potent 2-Aryl-6,7-dihydro-5 H-pyrrolo[1,2- a]imidazoles as WDR5-WIN-Site Inhibitors Using Fragment-Based Methods and Structure-Based Design.
J. Med. Chem., 61, 2018
7AXS
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BU of 7axs by Molmil
Structural characterisation of WDR5:CS-VIP8 interaction in cis state 1
分子名称: CS-VIP8, (ALQ)(4FO)R(ABA)(DPN)(EDN)(S7Z), WD repeat-containing protein 5
著者Werel, L, Essen, L.-O.
登録日2020-11-10
公開日2021-12-15
最終更新日2024-07-10
実験手法X-RAY DIFFRACTION (1.88 Å)
主引用文献Bistable Photoswitch Allows in Vivo Control of Hematopoiesis.
Acs Cent.Sci., 8, 2022
2H6K
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Histone H3 recognition and presentation by the WDR5 module of the MLL1 complex
分子名称: Histone H3 K4-Me 9-residue peptide, WD-repeat protein 5
著者Ruthenburg, A.J, Wang, W.-K, Graybosch, D.M, Li, H, Allis, C.D, Patel, D.J, Verdine, G.L.
登録日2006-05-31
公開日2006-07-04
最終更新日2023-08-30
実験手法X-RAY DIFFRACTION (1.89 Å)
主引用文献Histone H3 recognition and presentation by the WDR5 module of the MLL1 complex.
Nat.Struct.Mol.Biol., 13, 2006
4Y7R
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Crystal structure of WDR5 in complex with MYC MbIIIb peptide
分子名称: 1,2-ETHANEDIOL, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, MYC MbIIIb peptide, ...
著者Sun, Q, Phan, J, Olejniczak, E.T, Thomas, L.R, Fesik, S.W, Tansey, W.P.
登録日2015-02-16
公開日2015-04-15
最終更新日2023-09-27
実験手法X-RAY DIFFRACTION (1.898 Å)
主引用文献Interaction with WDR5 Promotes Target Gene Recognition and Tumorigenesis by MYC.
Mol.Cell, 58, 2015
6DY7
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WDR5 in complex with a WIN site inhibitor
分子名称: DIMETHYL SULFOXIDE, N-[3-(2,4-dichlorophenoxy)propyl]-1H-imidazol-2-amine, SULFATE ION, ...
著者Phan, J, Wang, F, Fesik, S.W.
登録日2018-07-01
公開日2019-03-13
最終更新日2024-03-13
実験手法X-RAY DIFFRACTION (1.9 Å)
主引用文献Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity.
Cell Rep, 26, 2019
2G99
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Structural basis for the specific recognition of methylated histone H3 lysine 4 by the WD-40 protein WDR5
分子名称: Histone H3, WD-repeat protein 5
著者Chai, J, Han, Z, Wang, H, Shen, Y.
登録日2006-03-06
公開日2006-09-06
最終更新日2023-10-25
実験手法X-RAY DIFFRACTION (1.9 Å)
主引用文献Structural basis for the specific recognition of methylated histone H3 lysine 4 by the WD-40 protein WDR5
To be published
8WXQ
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Structure of WDR5 in complex with WIN motif containing MBD3C
分子名称: GLY-ALA-ALA-ARG-CYS-ARG-VAL-PHE-SER-PRO, WD repeat-containing protein 5
著者Xu, L, Yang, Y.
登録日2023-10-30
公開日2024-06-26
実験手法X-RAY DIFFRACTION (1.9 Å)
主引用文献Structural studies of WDR5 in complex with MBD3C WIN motif reveal a unique binding mode.
J.Biol.Chem., 2024
7U9Y
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WDR5 bound to 2-(3,5-dimethoxybenzyl)-7-((2-methyl-1H-imidazol-1-yl)methyl)-5-(1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)-3,4-dihydroisoquinolin-1(2H)-one
分子名称: (5P)-2-[(3,5-dimethoxyphenyl)methyl]-7-[(2-methyl-1H-imidazol-1-yl)methyl]-5-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-3,4-dihydroisoquinolin-1(2H)-one, BENZAMIDINE, WD repeat-containing protein 5
著者Rietz, T.
登録日2022-03-11
公開日2022-04-27
最終更新日2023-10-18
実験手法X-RAY DIFFRACTION (1.9 Å)
主引用文献Discovery of Potent Orally Bioavailable WD Repeat Domain 5 (WDR5) Inhibitors Using a Pharmacophore-Based Optimization.
J.Med.Chem., 65, 2022
2O9K
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WDR5 in Complex with Dimethylated H3K4 Peptide
分子名称: H3 HISTONE, WD repeat protein 5
著者Min, J.R, Schuetz, A, Allali-Hassani, A, Martin, F, Loppnau, P, Vedadi, M, Weigelt, J, Sundstrom, M, Edwards, A.M, Arrowsmith, C.H, Bochkarev, A, Plotnikov, A.N, Structural Genomics Consortium (SGC)
登録日2006-12-13
公開日2006-12-19
最終更新日2023-12-27
実験手法X-RAY DIFFRACTION (1.9 Å)
主引用文献Structural Basis for Molecular Recognition and Presentation of Histone H3 by Wdr5.
Embo J., 25, 2006
4A7J
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Symmetric Dimethylation of H3 Arginine 2 is a Novel Histone Mark that Supports Euchromatin Maintenance
分子名称: HISTONE H3.1T, WD REPEAT-CONTAINING PROTEIN 5
著者Migliori, V, Muller, J, Phalke, S, Low, D, Bezzi, M, ChuenMok, W, Gunaratne, J, Capasso, P, Bassi, C, Cecatiello, V, DeMarco, A, Blackstock, W, Kuznetsov, V, Amati, B, Mapelli, M, Guccione, E.
登録日2011-11-14
公開日2012-01-11
最終更新日2023-12-20
実験手法X-RAY DIFFRACTION (1.9 Å)
主引用文献Symmetric Dimethylation of H3R2 is a Newly Identified Histone Mark that Supports Euchromatin Maintenance
Nat.Struct.Mol.Biol., 19, 2012
2H9M
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WDR5 in complex with unmodified H3K4 peptide
分子名称: H3 histone, WD-repeat protein 5
著者Min, J.R, Schuetz, A, Allali-Hassani, A, Martin, F, Loppnau, P, Vedadi, M, Weigelt, J, Sundstrom, M, Edwards, A.M, Arrowsmith, C.H, Bochkarev, A, Plotnikov, A.N, Structural Genomics Consortium (SGC)
登録日2006-06-10
公開日2006-08-01
最終更新日2024-02-14
実験手法X-RAY DIFFRACTION (1.9 Å)
主引用文献Structural basis for molecular recognition and presentation of histone H3 By WDR5.
Embo J., 25, 2006

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