8HMX
 
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3PSL
 | | Fine-tuning the stimulation of MLL1 methyltransferase activity by a histone H3 based peptide mimetic | | 分子名称: | N-alpha acetylated form of histone H3, WD repeat-containing protein 5 | | 著者 | Avdic, V, Zhang, P, Lanouette, S, Voronova, A, Skerjanc, I, Couture, J.-F. | | 登録日 | 2010-12-01 | | 公開日 | 2010-12-22 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | | 主引用文献 | Fine-tuning the stimulation of MLL1 methyltransferase activity by a histone H3-based peptide mimetic.
Faseb J., 25, 2011
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7JTO
 | | Crystal structure of Protac MS33 in complex with the WD repeat-containing protein 5 and pVHL:ElonginC:ElonginB | | 分子名称: | 1,2-ETHANEDIOL, 3-methyl-N-(11-{[2-(4-{[4'-(4-methylpiperazin-1-yl)-3'-{[6-oxo-4-(trifluoromethyl)-5,6-dihydropyridine-3-carbonyl]amino}[1,1'-biphenyl]-3-yl]methyl}piperazin-1-yl)ethyl]amino}-11-oxoundecanoyl)-L-valyl-(4R)-4-hydroxy-N-{[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}-L-prolinamide, Elongin-B, ... | | 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 (1.7 Å) | | 主引用文献 | A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models.
Sci Transl Med, 13, 2021
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8T5I
 | | Crystal structure of human WDR5 in complex with MR4397 | | 分子名称: | 1,2-ETHANEDIOL, DI(HYDROXYETHYL)ETHER, N-[(2S)-1-(6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)-1-oxopentan-2-yl]-3-[(1H-imidazol-1-yl)methyl]benzamide, ... | | 著者 | Kimani, S, Dong, A, Li, F, Loppnau, P, Ackloo, S, Vedadi, M, Brown, P.J, Arrowsmith, C.H, Edwards, A.M, Halabelian, L, Structural Genomics Consortium (SGC) | | 登録日 | 2023-06-13 | | 公開日 | 2023-08-09 | | 最終更新日 | 2024-05-22 | | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | | 主引用文献 | Crystal structure of human WDR5 in complex with MR4397
To be published
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4ESG
 | | X-ray structure of WDR5-MLL1 Win motif peptide binary complex | | 分子名称: | Histone-lysine N-methyltransferase MLL, WD repeat-containing protein 5 | | 著者 | Dharmarajan, V, Lee, J.-H, Patel, A, Skalnik, D.G, Cosgrove, M.S. | | 登録日 | 2012-04-23 | | 公開日 | 2012-05-30 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (1.7 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
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3EG6
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6PGB
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5EAP
 | | Crystal structure of human WDR5 in complex with compound 9e | | 分子名称: | 1,2-ETHANEDIOL, CHLORIDE ION, GLYCEROL, ... | | 著者 | DONG, A, DOMBROVSKI, L, SMIL, D, GETLIK, M, BOLSHAN, Y, WALKER, J.R, SENISTERRA, G, PODA, G, AL-AWAR, R, SCHAPIRA, M, VEDADI, M, Bountra, C, Edwards, A.M, Arrowsmith, C.H, BROWN, P.J, WU, H, Structural Genomics Consortium (SGC) | | 登録日 | 2015-10-16 | | 公開日 | 2015-11-04 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (1.73 Å) | | 主引用文献 | Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1).
J. Med. Chem., 59, 2016
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6UJJ
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6PG9
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4ERZ
 | | X-ray structure of WDR5-MLL4 Win motif peptide binary complex | | 分子名称: | Histone-lysine N-methyltransferase MLL4, 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 (1.75 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
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2H9L
 | | WDR5delta23 | | 分子名称: | SULFATE ION, 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 (1.75 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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6PGE
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8X3R
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7AXX
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2H68
 | | Histone H3 recognition and presentation by the WDR5 module of the MLL1 complex | | 分子名称: | 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 | 2006-05-30 | | 公開日 | 2006-07-04 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (1.79 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
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3UVN
 | | Crystal structure of WDR5 in complex with the WDR5-interacting motif of SET1A | | 分子名称: | Histone-lysine N-methyltransferase SETD1A, 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 (1.792 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
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5EAL
 | | Crystal structure of human WDR5 in complex with compound 9h | | 分子名称: | 1,2-ETHANEDIOL, 3-methyl-~{N}-[2-(4-methylpiperazin-1-yl)-5-quinolin-3-yl-phenyl]benzamide, CHLORIDE ION, ... | | 著者 | DONG, A, DOMBROVSKI, L, SMIL, D, GETLIK, M, BOLSHAN, Y, WALKER, J.R, SENISTERRA, G, PODA, G, AL-AWAR, R, SCHAPIRA, M, VEDADI, M, Bountra, C, Edwards, A.M, Arrowsmith, C.H, BROWN, P.J, WU, H, Structural Genomics Consortium (SGC) | | 登録日 | 2015-10-16 | | 公開日 | 2015-11-04 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Crystal structure of human WDR5 in complex with compound 9h
to be published
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6DAS
 | | 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: | N-[(1R)-6-(6,7-dihydro-5H-pyrrolo[1,2-a]imidazol-2-yl)-2,3-dihydro-1H-inden-1-yl]-3-methoxy-4-methylbenzamide, WD repeat-containing protein 5 | | 著者 | Phan, J, Fesik, S.W. | | 登録日 | 2018-05-01 | | 公開日 | 2018-07-18 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.8 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
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6U5M
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4QQE
 | | Crystal structure of WDR5, WD repeat domain 5 in complex with compound SGC-DS-MT-0345 | | 分子名称: | 1,2-ETHANEDIOL, CHLORIDE ION, N-[2-(4-methylpiperazin-1-yl)-5-(quinolin-3-yl)phenyl]-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide, ... | | 著者 | Dong, A, Dombrovski, L, Wernimont, A, Smil, D, Getlik, M, Senisterra, G, Poda, G, Al-Awar, R, Bountra, C, Arrowsmith, C.H, Edwards, A.M, Brown, P.J, Schapira, M, Vedadi, M, Wu, H, Structural Genomics Consortium (SGC) | | 登録日 | 2014-06-27 | | 公開日 | 2014-07-30 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Crystal structure of WDR5, WD repeat domain 5 in complex with compound SGC-DS-MT-0345
To be Published
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5EAM
 | | Crystal structure of human WDR5 in complex with compound 9o | | 分子名称: | 1,2-ETHANEDIOL, 2-[BIS-(2-HYDROXY-ETHYL)-AMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, SULFATE ION, ... | | 著者 | DONG, A, DOMBROVSKI, L, SMIL, D, GETLIK, M, BOLSHAN, Y, WALKER, J.R, SENISTERRA, G, PODA, G, AL-AWAR, R, SCHAPIRA, M, VEDADI, M, Bountra, C, Edwards, A.M, Arrowsmith, C.H, BROWN, P.J, WU, H, Structural Genomics Consortium (SGC) | | 登録日 | 2015-10-16 | | 公開日 | 2015-11-04 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1).
J. Med. Chem., 59, 2016
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8G3C
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8BB3
 | | 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
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3UR4
 | | Crystal structure of human WD repeat domain 5 with compound | | 分子名称: | 1,2-ETHANEDIOL, CHLORIDE ION, SULFATE ION, ... | | 著者 | Dong, A, Dombrovski, L, Senisterra, G, Wernimont, A, Wasney, G.A, Allali Hassani, A, Nguyen, K.T, Smil, D, Bolshan, Y, Hajian, T, Poda, G, Chau, I, Al-Awar, R, Bountra, C, Weigelt, J, Edwards, A.M, Arrowsmith, C.H, Brown, P, Schapira, M, Vedadi, M, Wu, H, Structural Genomics Consortium (SGC) | | 登録日 | 2011-11-21 | | 公開日 | 2011-12-14 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5.
Biochem. J., 449, 2013
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