4QL1
| Crystal structure of human WDR5 in complex with compound OICR-9429 | Descriptor: | 1,2-ETHANEDIOL, GLYCEROL, N-(4-(4-methylpiperazin-1-yl)-3'-(morpholinomethyl)-[1,1'-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide, ... | Authors: | Dong, A, Dombrovski, L, Walker, J.R, Getlik, M, Kuznetsova, E, Smil, D, Barsyte, D, Li, F, Poda, G, Senisterra, G, Marcellus, R, Al-Awar, R, Bountra, C, Arrowsmith, C.H, Edwards, A.M, Brown, P.J, Schapira, M, Vedadi, M, Wu, H, Structural Genomics Consortium (SGC) | Deposit date: | 2014-06-10 | Release date: | 2014-12-17 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (1.5 Å) | Cite: | Pharmacological targeting of the Wdr5-MLL interaction in C/EBP alpha N-terminal leukemia. Nat.Chem.Biol., 11, 2015
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4QQE
| Crystal structure of WDR5, WD repeat domain 5 in complex with compound SGC-DS-MT-0345 | Descriptor: | 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, ... | Authors: | 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) | Deposit date: | 2014-06-27 | Release date: | 2014-07-30 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Crystal structure of WDR5, WD repeat domain 5 in complex with compound SGC-DS-MT-0345 To be Published
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3N0D
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5EAP
| Crystal structure of human WDR5 in complex with compound 9e | Descriptor: | 1,2-ETHANEDIOL, CHLORIDE ION, GLYCEROL, ... | Authors: | 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) | Deposit date: | 2015-10-16 | Release date: | 2015-11-04 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.73 Å) | Cite: | 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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3MXX
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5EAR
| Crystal structure of human WDR5 in complex with compound 9d | Descriptor: | 1,2-ETHANEDIOL, N-[5-(2,3-dihydro-1-benzofuran-7-yl)-2-(4-methylpiperazin-1-yl)phenyl]-3-methylbenzamide, SULFATE ION, ... | Authors: | 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) | Deposit date: | 2015-10-16 | Release date: | 2015-11-04 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | 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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3N0E
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5EAL
| Crystal structure of human WDR5 in complex with compound 9h | Descriptor: | 1,2-ETHANEDIOL, 3-methyl-~{N}-[2-(4-methylpiperazin-1-yl)-5-quinolin-3-yl-phenyl]benzamide, CHLORIDE ION, ... | Authors: | 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) | Deposit date: | 2015-10-16 | Release date: | 2015-11-04 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Crystal structure of human WDR5 in complex with compound 9h to be published
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5EAM
| Crystal structure of human WDR5 in complex with compound 9o | Descriptor: | 1,2-ETHANEDIOL, 2-[BIS-(2-HYDROXY-ETHYL)-AMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, SULFATE ION, ... | Authors: | 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) | Deposit date: | 2015-10-16 | Release date: | 2015-11-04 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | 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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3ODT
| Crystal structure of WD40 beta propeller domain of Doa1 | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, Protein DOA1 | Authors: | Pashkova, N, Gakhar, L, Winistorfer, S.C, Yu, L, Ramaswamy, S, Piper, R.C. | Deposit date: | 2010-08-11 | Release date: | 2010-12-01 | Last modified: | 2019-12-25 | Method: | X-RAY DIFFRACTION (1.35 Å) | Cite: | WD40 Repeat Propellers Define a Ubiquitin-Binding Domain that Regulates Turnover of F Box Proteins. Mol.Cell, 40, 2010
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3OW8
| Crystal Structure of the WD repeat-containing protein 61 | Descriptor: | UNKNOWN ATOM OR ION, WD repeat-containing protein 61 | Authors: | Tempel, W, Li, Z, Chao, X, Lam, R, Wernimont, A.K, He, H, Seitova, A, Pan, P.W, Li, Y, Bountra, C, Weigelt, J, Arrowsmith, C.H, Edwards, A.M, Bochkarev, A, Min, J, Structural Genomics Consortium (SGC) | Deposit date: | 2010-09-17 | Release date: | 2010-09-29 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Structure and function of WD40 domain proteins. Protein Cell, 2, 2011
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3P4F
| Structural and biochemical insights into MLL1 core complex assembly and regulation. | Descriptor: | Histone-lysine N-methyltransferase MLL, Retinoblastoma-binding protein 5, WD repeat-containing protein 5 | Authors: | Avdic, V, Zhang, P, Lanouette, S, Groulx, A, Tremblay, V, Brunzelle, J.B, Couture, J.-F. | Deposit date: | 2010-10-06 | Release date: | 2010-12-08 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.35 Å) | Cite: | Structural and biochemical insights into MLL1 core complex assembly. Structure, 19, 2011
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6IAM
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5H13
| EED in complex with PRC2 allosteric inhibitor EED396 | Descriptor: | 4-azanylidene-2-(3-methoxy-4-propan-2-yloxy-phenyl)-6,7-dihydro-[1,3]benzodioxolo[6,5-a]quinolizine-3-carbonitrile, GLYCEROL, PRASEODYMIUM ION, ... | Authors: | Zhao, K, Zhao, M, Luo, X, Zhang, H. | Deposit date: | 2016-10-08 | Release date: | 2017-01-25 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED PLoS ONE, 12, 2017
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5HQG
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5I2T
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5IGO
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5YZV
| Biophysical and structural characterization of the thermostable WD40 domain of a prokaryotic protein, Thermomonospora curvata PkwA | Descriptor: | Probable serine/threonine-protein kinase PkwA | Authors: | Li, D.Y, Shen, C, Du, Y, Qiao, F.F, Kong, T, Yuan, L.R, Zhang, D.L, Wu, X.H, Wu, Y.D. | Deposit date: | 2017-12-15 | Release date: | 2018-10-03 | Last modified: | 2024-03-27 | Method: | X-RAY DIFFRACTION (2.6 Å) | Cite: | Biophysical and structural characterization of the thermostable WD40 domain of a prokaryotic protein, Thermomonospora curvata PkwA Sci Rep, 8, 2018
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5IGQ
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6B3X
| Crystal structure of CstF-50 in complex with CstF-77 | Descriptor: | Cleavage stimulation factor subunit 1, Cleavage stimulation factor subunit 3 | Authors: | Yang, W, Hsu, P, Yang, F, Song, J.E, Varani, G. | Deposit date: | 2017-09-25 | Release date: | 2017-11-29 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Reconstitution of the CstF complex unveils a regulatory role for CstF-50 in recognition of 3'-end processing signals. Nucleic Acids Res., 46, 2018
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6BYN
| Crystal structure of WDR5-Mb(S4) monobody complex | Descriptor: | WD repeat-containing protein 5, WDR5-binding Monobody, Mb(S4) | Authors: | Gupta, A, Koide, S. | Deposit date: | 2017-12-21 | Release date: | 2018-07-04 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.69 Å) | Cite: | Facile target validation in an animal model with intracellularly expressed monobodies. Nat. Chem. Biol., 14, 2018
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5SXM
| WDR5 in complex with MLL Win motif peptidomimetic | Descriptor: | ACE-ALA-ARG-THR-GLU-VAL-TYR-NH2, WD repeat-containing protein 5 | Authors: | Alicea-Velazquez, N.L, Shinsky, S.A, Cosgrove, M.S. | Deposit date: | 2016-08-09 | Release date: | 2016-09-07 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | 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
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5TF2
| CRYSTAL STRUCTURE OF THE WD40 DOMAIN OF THE HUMAN PROLACTIN REGULATORY ELEMENT-BINDING PROTEIN | Descriptor: | Prolactin regulatory element-binding protein, UNKNOWN ATOM OR ION | Authors: | Walker, J.R, Zhang, Q, Dong, A, Wernimont, A, Li, Y, He, H, Tempel, W, Bountra, C, Edwards, A.M, Arrowsmith, C.H, Chen, Z, Tong, Y, Structural Genomics Consortium (SGC) | Deposit date: | 2016-09-23 | Release date: | 2016-11-23 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | CRYSTAL STRUCTURE OF THE WD40 DOMAIN OF THE HUMAN PROLACTIN REGULATORY ELEMENT-BINDING PROTEIN (CASP target) To be published
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5U8F
| Polycomb protein EED in complex with inhibitor: (3R,4S)-1-[(1S)-7-fluoro-2,3-dihydro-1H-inden-1-yl]-N,N-dimethyl-4-(1-methyl-1H-indol-3-yl)pyrrolidin-3-amine | Descriptor: | (3R,4S)-1-[(1S)-7-fluoro-2,3-dihydro-1H-inden-1-yl]-N,N-dimethyl-4-(1-methyl-1H-indol-3-yl)pyrrolidin-3-amine, Polycomb protein EED | Authors: | Jakob, C.G, Zhu, H. | Deposit date: | 2016-12-14 | Release date: | 2017-03-15 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (1.343 Å) | Cite: | SAR of amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex through EED binding. Bioorg. Med. Chem. Lett., 27, 2017
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5U5H
| Crystal structure of EED in complex with 6-(2-fluoro-5-methoxybenzyl)-1-isopropyl-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-3-amine 6-(2-fluoro-5-methoxybenzyl)-1-isopropyl-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-3-amine | Descriptor: | (6S)-6-[(2-fluoro-5-methoxyphenyl)methyl]-1-(propan-2-yl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-3-amine, GLYCEROL, Polycomb protein EED | Authors: | Bussiere, D, Shu, W. | Deposit date: | 2016-12-06 | Release date: | 2017-01-11 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase. J. Med. Chem., 60, 2017
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