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PDB: 157 件

4ERQ
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X-ray structure of WDR5-MLL2 Win motif peptide binary complex
分子名称: Histone-lysine N-methyltransferase MLL2, WD repeat-containing protein 5
著者Dharmarajan, V, Lee, J.-H, Patel, A, Skalnik, D.G, Cosgrove, M.S.
登録日2012-04-20
公開日2012-05-16
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (1.906 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
2H9P
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WDR5 in complex with trimethylated 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2011-07-13
実験手法X-RAY DIFFRACTION (1.91 Å)
主引用文献Structural basis for molecular recognition and presentation of histone H3 By WDR5.
Embo J., 25, 2006
6OI0
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Crystal structure of human WDR5 in complex with L-arginine
分子名称: ARGININE, GLYCEROL, SULFATE ION, ...
著者Lorton, B.M, Harijan, R.K, Burgos, E, Bonanno, J.B, Almo, S.C, Shechter, D.
登録日2019-04-08
公開日2020-04-01
最終更新日2023-10-11
実験手法X-RAY DIFFRACTION (1.92 Å)
主引用文献A Binary Arginine Methylation Switch on Histone H3 Arginine 2 Regulates Its Interaction with WDR5.
Biochemistry, 59, 2020
5M23
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Modulation of MLL1 Methyltransferase Activity
分子名称: 4-[(~{E})-[4-[[[(2~{S})-2-[[(2~{S})-2-[[(2~{S})-2-[[(2~{S})-2-azanyl-3-oxidanyl-propanoyl]amino]propanoyl]amino]-5-carbamimidamido-pentanoyl]amino]propanoyl]amino]methyl]phenyl]diazenyl]-~{N}-[(2~{S})-3-methyl-1-oxidanylidene-butan-2-yl]benzamide, WD repeat-containing protein 5
著者Srinivasan, V.
登録日2016-10-11
公開日2017-06-28
最終更新日2024-01-17
実験手法X-RAY DIFFRACTION (1.97 Å)
主引用文献Controlled inhibition of methyltransferases using photoswitchable peptidomimetics: towards an epigenetic regulation of leukemia.
Chem Sci, 8, 2017
6PG5
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WDR5delta32 bound to benzyl (4-(5-(hydroxymethyl)-1H-imidazol-2-yl)butyl)carbamate
分子名称: SULFATE ION, WD repeat-containing protein 5, benzyl {4-[5-(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 (1.99 Å)
主引用文献Fragment screening for a protein-protein interaction inhibitor to WDR5.
Struct Dyn., 6, 2019
4CY2
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Crystal structure of the KANSL1-WDR5-KANSL2 complex.
分子名称: KAT8 REGULATORY NSL COMPLEX SUBUNIT 1, KAT8 REGULATORY NSL COMPLEX SUBUNIT 2, WD REPEAT-CONTAINING PROTEIN 5
著者Dias, J, Brettschneider, J, Cusack, S, Kadlec, J.
登録日2014-04-09
公開日2014-05-14
最終更新日2023-12-20
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Structural Analysis of the Kansl1/Wdr5/Kansl2 Complex Reveals that Wdr5 is Required for Efficient Assembly and Chromatin Targeting of the Nsl Complex.
Genes Dev., 28, 2014
5SXM
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WDR5 in complex with MLL Win motif peptidomimetic
分子名称: ACE-ALA-ARG-THR-GLU-VAL-TYR-NH2, WD repeat-containing protein 5
著者Alicea-Velazquez, N.L, Shinsky, S.A, Cosgrove, M.S.
登録日2016-08-09
公開日2016-09-07
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Targeted Disruption of the Interaction between WD-40 Repeat Protein 5 (WDR5) and Mixed Lineage Leukemia (MLL)/SET1 Family Proteins Specifically Inhibits MLL1 and SETd1A Methyltransferase Complexes.
J.Biol.Chem., 291, 2016
2H9N
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WDR5 in complex with monomethylated 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2011-07-13
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Structural basis for molecular recognition and presentation of histone H3 By WDR5.
Embo J., 25, 2006
8UJY
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Crystal structure of human WD repeat-containing protein 5 in complex with 4-(3,5-dimethoxybenzyl)-9-(4-fluoro-2-methylphenyl)-7-((2-imino-3-methyl-2,3-dihydro-1H-imidazol-1-yl)methyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one (compound 8)
分子名称: (9P)-4-[(3,5-dimethoxyphenyl)methyl]-9-(4-fluoro-2-methylphenyl)-7-{[(2E)-2-imino-3-methyl-2,3-dihydro-1H-imidazol-1-yl]methyl}-3,4-dihydro-1,4-benzoxazepin-5(2H)-one, WD repeat-containing protein 5
著者Zhao, B, Amporndanai, K, Fesik, S.W.
登録日2023-10-11
公開日2023-12-20
最終更新日2024-01-10
実験手法X-RAY DIFFRACTION (2.01 Å)
主引用文献Structure-Based Discovery of Potent, Orally Bioavailable Benzoxazepinone-Based WD Repeat Domain 5 Inhibitors.
J.Med.Chem., 66, 2023
6UFX
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WD repeat-containing protein 5 complexed with N-[(3,5-dimethoxyphenyl)methyl]-4'-fluoro-5-{[(2E)-2-imino-3-methyl-2,3-dihydro-1H-imidazol-1-yl]methyl}-2'-methyl[1,1'-biphenyl]-3-carboxamide (compound 13)
分子名称: N-[(3,5-dimethoxyphenyl)methyl]-4'-fluoro-5-{[(2E)-2-imino-3-methyl-2,3-dihydro-1H-imidazol-1-yl]methyl}-2'-methyl[1,1'-biphenyl]-3-carboxamide, WD repeat-containing protein 5
著者Rietz, T.A, Fesik, S.W, Zhao, B.
登録日2019-09-25
公開日2020-01-01
最終更新日2023-10-11
実験手法X-RAY DIFFRACTION (2.015 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
7DNO
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Characterization of Peptide Ligands Against WDR5 Isolated Using Phage Display Technique
分子名称: CYS-ARG-THR-LEU-PRO-PHE, WD repeat-containing protein 5
著者Cao, J, Cao, D, Xiong, B, Li, Y, Fan, T.
登録日2020-12-10
公開日2021-02-10
最終更新日2023-11-29
実験手法X-RAY DIFFRACTION (2.03 Å)
主引用文献Phage-Display Based Discovery and Characterization of Peptide Ligands against WDR5.
Molecules, 26, 2021
6PG3
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WDR5delta23 bound to (2-butyl-1H-imidazol-4-yl)methanol
分子名称: (2-butyl-1H-imidazol-4-yl)methanol, WD repeat-containing protein 5
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 (2.04 Å)
主引用文献Fragment screening for a protein-protein interaction inhibitor to WDR5.
Struct Dyn., 6, 2019
3MXX
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Crystal structure of WDR5 mutant (S62A)
分子名称: WD repeat-containing protein 5
著者Wu, Y.-D, Wu, X.-H, Gao, Y, Chen, R.-C.
登録日2010-05-08
公開日2010-10-20
最終更新日2023-11-01
実験手法X-RAY DIFFRACTION (2.05 Å)
主引用文献The Effect of Asp-His-Ser/Thr-Trp Tetrad on the Thermostability of WD40-Repeat Proteins
Biochemistry, 49, 2010
8BB2
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Structure of human WDR5 and pVHL:ElonginC:ElonginB bound to PROTAC with PEG linker (conformation #2)
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 (2.05 Å)
主引用文献Structure of human WDR5 and pVHL:ElonginC:ElonginB bound to PROTAC with PEG linker (conformation #2)
To Be Published
8WXR
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Structure of WDR5 in complex with WIN motif containing MBD3C F47A
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
最終更新日2024-07-17
実験手法X-RAY DIFFRACTION (2.08 Å)
主引用文献Structural studies of WDR5 in complex with MBD3C WIN motif reveal a unique binding mode.
J.Biol.Chem., 300, 2024
8WXX
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Structure of WDR5 in complex with WIN motif containing SET1B E1750R/G1751V
分子名称: SET1B, WD repeat-containing protein 5
著者Xu, L, Yang, Y.
登録日2023-10-30
公開日2024-06-26
最終更新日2024-07-17
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献Structural studies of WDR5 in complex with MBD3C WIN motif reveal a unique binding mode.
J.Biol.Chem., 300, 2024
4GM9
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Crystal structure of human WD repeat domain 5 with compound MM-401
分子名称: MM-401, WD repeat-containing protein 5
著者Karatas, H, Townsend, E.C, Chen, Y, Bernard, D, Liu, L, Dou, Y, Lei, M, Wang, S.
登録日2012-08-15
公開日2014-02-19
最終更新日2023-11-15
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献Crystal structure of human WD repeat domain 5 with compound MM-401
To be Published
2CNX
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WDR5 and Histone H3 Lysine 4 dimethyl complex at 2.1 angstrom
分子名称: HISTONE H3 DIMETHYL-LYSINE 4, WD-REPEAT PROTEIN 5
著者Ruthenburg, A.J, Wang, W, Graybosch, D.M, Li, H, Allis, C.D, Patel, D.J, Verdine, G.L.
登録日2006-05-25
公開日2006-07-03
最終更新日2023-12-13
実験手法X-RAY DIFFRACTION (2.1 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
7JTP
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Crystal structure of Protac MS67 in complex with the WD repeat-containing protein 5 and pVHL:ElonginC:ElonginB
分子名称: Elongin-B, Elongin-C, GLYCEROL, ...
著者Kottur, J, Jain, R, Aggarwal, A.K.
登録日2020-08-18
公開日2021-10-06
最終更新日2023-10-18
実験手法X-RAY DIFFRACTION (2.12 Å)
主引用文献A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models.
Sci Transl Med, 13, 2021
8F1G
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Crystal structure of human WDR5 in complex with compound WM662
分子名称: (2S)-2-({(2S)-3-(3'-chloro[1,1'-biphenyl]-4-yl)-1-oxo-1-[(1H-tetrazol-5-yl)amino]propan-2-yl}oxy)propanoic acid, GLYCEROL, SULFATE ION, ...
著者Liu, H.
登録日2022-11-05
公開日2023-01-11
最終更新日2023-10-25
実験手法X-RAY DIFFRACTION (2.14 Å)
主引用文献Discovery of Potent Small-Molecule Inhibitors of WDR5-MYC Interaction.
Acs Chem.Biol., 18, 2023
8BB5
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Structure of human WDR5 and pVHL:ElonginC:ElonginB bound to PROTAC with Aryl linker
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 (2.2 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
3UVO
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Crystal structure of WDR5 in complex with the WDR5-interacting motif of SET1B
分子名称: Histone-lysine N-methyltransferase SETD1B, WD repeat-containing protein 5
著者Zhang, P, Lee, H, Brunzelle, J.S, Couture, J.-F.
登録日2011-11-30
公開日2011-12-14
最終更新日2023-09-13
実験手法X-RAY DIFFRACTION (2.2 Å)
主引用文献The plasticity of WDR5 peptide-binding cleft enables the binding of the SET1 family of histone methyltransferases.
Nucleic Acids Res., 40, 2012
3UVL
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Crystal structure of WDR5 in complex with the WDR5-interacting motif of MLL3
分子名称: Histone-lysine N-methyltransferase MLL3, WD repeat-containing protein 5
著者Zhang, P, Lee, H, Brunzelle, J.S, Couture, J.-F.
登録日2011-11-30
公開日2011-12-14
最終更新日2023-09-13
実験手法X-RAY DIFFRACTION (2.2 Å)
主引用文献The plasticity of WDR5 peptide-binding cleft enables the binding of the SET1 family of histone methyltransferases.
Nucleic Acids Res., 40, 2012
2CO0
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WDR5 and unmodified Histone H3 complex at 2.25 Angstrom
分子名称: HISTONE H3 DIMETHYL-LYSINE 4, WD-REPEAT PROTEIN 5
著者Ruthenburg, A.J, Wang, W, Graybosch, D.M, Li, H, Allis, C.D, Patel, D.J, Verdine, G.L.
登録日2006-05-25
公開日2006-07-03
最終更新日2023-12-13
実験手法X-RAY DIFFRACTION (2.25 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
3N0D
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Crystal structure of WDR5 mutant (W330F)
分子名称: WD repeat-containing protein 5
著者Wu, Y.-D, Wu, X.-H, Gao, Y, Chen, R.-C.
登録日2010-05-13
公開日2010-10-20
最終更新日2023-11-01
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献The Effect of Asp-His-Ser/Thr-Trp Tetrad on the Thermostability of WD40-Repeat Proteins
Biochemistry, 49, 2010

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