5VFC
| WDR5 bound to inhibitor MM-589 | Descriptor: | 1,2-ETHANEDIOL, N-{(3R,6S,9S,12R)-6-ethyl-12-methyl-9-[3-(N'-methylcarbamimidamido)propyl]-2,5,8,11-tetraoxo-3-phenyl-1,4,7,10-tetraazacyclotetradecan-12-yl}-2-methylpropanamide, SULFATE ION, ... | Authors: | Stuckey, J.A. | Deposit date: | 2017-04-07 | Release date: | 2017-06-28 | Last modified: | 2024-03-13 | Method: | X-RAY DIFFRACTION (1.64 Å) | Cite: | Discovery of a Highly Potent, Cell-Permeable Macrocyclic Peptidomimetic (MM-589) Targeting the WD Repeat Domain 5 Protein (WDR5)-Mixed Lineage Leukemia (MLL) Protein-Protein Interaction. J. Med. Chem., 60, 2017
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5WP3
| Crystal Structure of EED in complex with EB22 | Descriptor: | EB22, Polycomb protein EED, UNKNOWN ATOM OR ION | Authors: | Dong, C, Tempel, W, Zhu, L, Moody, J.D, Baker, D, Bountra, C, Arrowsmith, C.H, Edwards, A.M, Min, J, Structural Genomics Consortium (SGC) | Deposit date: | 2017-08-03 | Release date: | 2017-09-13 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.55 Å) | Cite: | First critical repressive H3K27me3 marks in embryonic stem cells identified using designed protein inhibitor. Proc. Natl. Acad. Sci. U.S.A., 114, 2017
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6OI0
| Crystal structure of human WDR5 in complex with L-arginine | Descriptor: | ARGININE, GLYCEROL, SULFATE ION, ... | Authors: | Lorton, B.M, Harijan, R.K, Burgos, E, Bonanno, J.B, Almo, S.C, Shechter, D. | Deposit date: | 2019-04-08 | Release date: | 2020-04-01 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (1.92 Å) | Cite: | A Binary Arginine Methylation Switch on Histone H3 Arginine 2 Regulates Its Interaction with WDR5. Biochemistry, 59, 2020
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6OI3
| Crystal structure of human WDR5 in complex with monomethyl H3R2 peptide | Descriptor: | GLYCEROL, Monomethyl H3R2 peptide, SULFATE ION, ... | Authors: | Lorton, B.M, Harijan, R.K, Burgos, E, Bonanno, J.B, Almo, S.C, Shechter, D. | Deposit date: | 2019-04-08 | Release date: | 2020-04-01 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (1.66 Å) | Cite: | A Binary Arginine Methylation Switch on Histone H3 Arginine 2 Regulates Its Interaction with WDR5. Biochemistry, 59, 2020
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6OI1
| Crystal structure of human WDR5 in complex with monomethyl L-arginine | Descriptor: | (2S)-2-amino-5-[(N-methylcarbamimidoyl)amino]pentanoic acid, GLYCEROL, SULFATE ION, ... | Authors: | Lorton, B.M, Harijan, R.K, Burgos, E, Bonanno, J.B, Almo, S.C, Shechter, D. | Deposit date: | 2019-04-08 | Release date: | 2020-04-01 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (1.68 Å) | Cite: | A Binary Arginine Methylation Switch on Histone H3 Arginine 2 Regulates Its Interaction with WDR5. Biochemistry, 59, 2020
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6OFZ
| Crystal structure of human WDR5 | Descriptor: | WD repeat-containing protein 5 | Authors: | Lorton, B.M, Harijan, R.K, Burgos, E, Bonanno, J.B, Almo, S.C, Shechter, D. | Deposit date: | 2019-04-01 | Release date: | 2020-04-01 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (1.85 Å) | Cite: | A Binary Arginine Methylation Switch on Histone H3 Arginine 2 Regulates Its Interaction with WDR5. Biochemistry, 59, 2020
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6OI2
| Crystal structure of human WDR5 in complex with symmetric dimethyl-L-arginine | Descriptor: | GLYCEROL, N3, N4-DIMETHYLARGININE, ... | Authors: | Lorton, B.M, Harijan, R.K, Burgos, E, Bonanno, J.B, Almo, S.C, Shechter, D. | Deposit date: | 2019-04-08 | Release date: | 2020-04-01 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (1.68 Å) | Cite: | A Binary Arginine Methylation Switch on Histone H3 Arginine 2 Regulates Its Interaction with WDR5. Biochemistry, 59, 2020
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6PGE
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6PGC
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6PG7
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6PGD
| WDR5delta32 bound to peptidomimetic | Descriptor: | N-acetyl-L-alanyl-5-[5-(hydroxymethyl)-1H-imidazol-2-yl]-L-norvalyl-L-valinamide, SULFATE ION, WD repeat-containing protein 5 | Authors: | Dennis, M.L, Peat, T.S. | Deposit date: | 2019-06-24 | Release date: | 2019-12-11 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (1.5 Å) | Cite: | Fragment screening for a protein-protein interaction inhibitor to WDR5. Struct Dyn., 6, 2019
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6PG6
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6PGF
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6PBG
| Crystal structure of WD-repeat domain of human coatomer subunit Alpha (COPA) | Descriptor: | Coatomer subunit alpha, L(+)-TARTARIC ACID, UNKNOWN ATOM OR ION | Authors: | Halabelian, L, Zeng, H, Dong, A, Loppnau, P, Seitova, A, Hutchinson, A, Bountra, C, Edwards, A.M, Arrowsmith, C.H, Structural Genomics Consortium (SGC) | Deposit date: | 2019-06-13 | Release date: | 2019-06-26 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (1.72 Å) | Cite: | Crystal structure of W repeat domain of human coatomer subunit Alpha (COPA) to be published
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6PG5
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6PGB
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6PG3
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6PG8
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6PG4
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6PG9
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6PGA
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6IAM
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7P3J
| EED in complex with compound 4 | Descriptor: | 8-[6-[(dimethylamino)methyl]-2-methyl-pyridin-3-yl]-5-[(5-fluoranyl-2,3-dihydro-1-benzofuran-4-yl)methylamino]-2H-pyrido[3,4-d]pyridazin-1-one, MAGNESIUM ION, N-(2,3-dihydro-1-benzofuran-4-ylmethyl)-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine, ... | Authors: | Read, J.A. | Deposit date: | 2021-07-07 | Release date: | 2021-12-08 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (1.93 Å) | Cite: | Diverse, Potent, and Efficacious Inhibitors That Target the EED Subunit of the Polycomb Repressive Complex 2 Methyltransferase. J.Med.Chem., 64, 2021
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7P3G
| EED in complex with compound 4 | Descriptor: | N-(2,3-dihydro-1-benzofuran-4-ylmethyl)-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine, N5-[(5-fluoranyl-2,3-dihydro-1-benzofuran-4-yl)methyl]-N8-methyl-N8-(1-methylpyrazol-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidine-5,8-diamine, Polycomb protein EED | Authors: | Read, J.A. | Deposit date: | 2021-07-07 | Release date: | 2021-12-08 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (2.39 Å) | Cite: | Diverse, Potent, and Efficacious Inhibitors That Target the EED Subunit of the Polycomb Repressive Complex 2 Methyltransferase. J.Med.Chem., 64, 2021
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7P3C
| EED in complex with compound 4 | Descriptor: | N-(2,3-dihydro-1-benzofuran-4-ylmethyl)-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine, N-[5-[(5-fluoranyl-2,3-dihydro-1-benzofuran-4-yl)methylamino]-[1,2,4]triazolo[4,3-c]pyrimidin-8-yl]benzamide, Polycomb protein EED | Authors: | Read, J.A. | Deposit date: | 2021-07-07 | Release date: | 2021-12-08 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (1.61 Å) | Cite: | Diverse, Potent, and Efficacious Inhibitors That Target the EED Subunit of the Polycomb Repressive Complex 2 Methyltransferase. J.Med.Chem., 64, 2021
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