8F93
 
 | | WDR5 covalently modified at Y228 by (R)-2-SF | | 分子名称: | 3-ethynyl-5-{[(3R)-4-{1-[(2-methoxyphenyl)methyl]-1H-benzimidazole-5-carbonyl}-3-methylpiperazin-1-yl]methyl}benzene-1-sulfonyl fluoride, CHLORIDE ION, GLYCEROL, ... | | 著者 | Taunton, J, Craven, G.B, Chen, Y. | | 登録日 | 2022-11-23 | | 公開日 | 2023-05-31 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Direct mapping of ligandable tyrosines and lysines in cells with chiral sulfonyl fluoride probes.
Nat.Chem., 15, 2023
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3P4F
 | | Structural and biochemical insights into MLL1 core complex assembly and regulation. | | 分子名称: | Histone-lysine N-methyltransferase MLL, Retinoblastoma-binding protein 5, WD repeat-containing protein 5 | | 著者 | Avdic, V, Zhang, P, Lanouette, S, Groulx, A, Tremblay, V, Brunzelle, J.B, Couture, J.-F. | | 登録日 | 2010-10-06 | | 公開日 | 2010-12-08 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.35 Å) | | 主引用文献 | Structural and biochemical insights into MLL1 core complex assembly.
Structure, 19, 2011
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8WXU
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8WXV
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5M25
 | | Modulation of MLL1 Methyltransferase Activity | | 分子名称: | (2~{S})-2-[[(2~{S})-2-[[(2~{S})-2-azanyl-3-oxidanyl-propanoyl]amino]propanoyl]amino]-5-carbamimidamido-~{N}-[(2~{S})-1-[[4-[(~{E})-[4-(hydroxymethyl)phenyl]diazenyl]phenyl]methylamino]-1-oxidanylidene-propan-2-yl]pentanamide, 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 (2.43 Å) | | 主引用文献 | Controlled inhibition of methyltransferases using photoswitchable peptidomimetics: towards an epigenetic regulation of leukemia.
Chem Sci, 8, 2017
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7AXP
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6PG7
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6PGA
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7Q2J
 | | Quaternary Complex of human WDR5 and pVHL:ElonginC:ElonginB bound to PROTAC Homer | | 分子名称: | Elongin-B, Elongin-C, N-[5-[4-[[5-[[(2S)-3,3-dimethyl-1-[(2S,4R)-2-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methylcarbamoyl]-4-oxidanyl-pyrrolidin-1-yl]-1-oxidanylidene-butan-2-yl]amino]-5-oxidanylidene-pentyl]carbamoyl]phenyl]-2-(4-methylpiperazin-1-yl)phenyl]-6-oxidanylidene-4-(trifluoromethyl)-1H-pyridine-3-carboxamide, ... | | 著者 | Kraemer, A, Doelle, A, Schwalm, M.P, Adhikari, B, Wolf, E, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2021-10-25 | | 公開日 | 2021-11-24 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (2.5 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
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3N0E
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6DYA
 | | WDR5 in complex with a WIN site inhibitor | | 分子名称: | DIMETHYL SULFOXIDE, N-[(3,5-dichlorophenyl)methyl]-3-[(1H-imidazol-1-yl)methyl]benzamide, 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 (2.56 Å) | | 主引用文献 | Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity.
Cell Rep, 26, 2019
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4GM8
 | | Crystal structure of human WD repeat domain 5 with compound MM-102 | | 分子名称: | MM-102, WD repeat-containing protein 5 | | 著者 | Karatas, H, Townsend, E.C, Chen, Y, Bernard, D, Cao, F, Liu, L, Lei, M, Dou, Y, Wang, S. | | 登録日 | 2012-08-15 | | 公開日 | 2013-07-31 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (2.601 Å) | | 主引用文献 | High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interaction.
J.Am.Chem.Soc., 135, 2013
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6BYN
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2G9A
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6WJQ
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4GMB
 | | Crystal structure of human WD repeat domain 5 with compound MM-402 | | 分子名称: | MM-402, WD repeat-containing protein 5 | | 著者 | Karatas, H, Townsend, E.C, Chen, Y, Bernard, D, Cao, F, Liu, L, Lei, M, Dou, Y, 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 (2.781 Å) | | 主引用文献 | 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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8BB4
 | | Structure of human WDR5 and pVHL:ElonginC:ElonginB bound to PROTAC with C3 linker | | 分子名称: | Elongin-B, Elongin-C, WD repeat-containing protein 5, ... | | 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 (2.8 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
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6KIU
 | | Cryo-EM structure of human MLL1-ubNCP complex (3.2 angstrom) | | 分子名称: | DNA (145-MER), GLUTAMINE, Histone H2A, ... | | 著者 | Huang, J, Xue, H, Yao, T. | | 登録日 | 2019-07-20 | | 公開日 | 2019-09-11 | | 最終更新日 | 2024-03-27 | | 実験手法 | ELECTRON MICROSCOPY (3.2 Å) | | 主引用文献 | Structural basis of nucleosome recognition and modification by MLL methyltransferases.
Nature, 573, 2019
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4GM3
 | | Crystal structure of human WD repeat domain 5 with compound MM-101 | | 分子名称: | MM-101, WD repeat-containing protein 5 | | 著者 | Karatas, H, Townsend, E.C, Chen, Y, Bernard, D, Cao, F, Liu, L, Lei, M, Dou, Y, Wang, S. | | 登録日 | 2012-08-15 | | 公開日 | 2013-07-31 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (3.393 Å) | | 主引用文献 | High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interaction.
J.Am.Chem.Soc., 135, 2013
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8DU4
 | | Complex between RbBP5-WDR5 and an H2B-ubiquitinated nucleosome | | 分子名称: | 601 DNA (146-MER), Histone H2A, Histone H2B 1.1, ... | | 著者 | Niklas, H.A, Rahman, S, Worden, E.J, Wolberger, C. | | 登録日 | 2022-07-26 | | 公開日 | 2022-09-21 | | 最終更新日 | 2022-10-05 | | 実験手法 | ELECTRON MICROSCOPY (3.55 Å) | | 主引用文献 | Multistate structures of the MLL1-WRAD complex bound to H2B-ubiquitinated nucleosome.
Proc.Natl.Acad.Sci.USA, 119, 2022
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6KIV
 | | Cryo-EM structure of human MLL1-ubNCP complex (4.0 angstrom) | | 分子名称: | DNA (145-MER), Histone H2A, Histone H2B 1.1, ... | | 著者 | Huang, J, Xue, H, Yao, T. | | 登録日 | 2019-07-20 | | 公開日 | 2019-09-11 | | 最終更新日 | 2024-03-27 | | 実験手法 | ELECTRON MICROSCOPY (4 Å) | | 主引用文献 | Structural basis of nucleosome recognition and modification by MLL methyltransferases.
Nature, 573, 2019
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6KIW
 | | Cryo-EM structure of human MLL3-ubNCP complex (4.0 angstrom) | | 分子名称: | DNA (144-MER), DNA (145-MER), Histone H2A, ... | | 著者 | Huang, J, Xue, H, Yao, T. | | 登録日 | 2019-07-20 | | 公開日 | 2019-09-11 | | 最終更新日 | 2024-03-27 | | 実験手法 | ELECTRON MICROSCOPY (4 Å) | | 主引用文献 | Structural basis of nucleosome recognition and modification by MLL methyltransferases.
Nature, 573, 2019
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6KIX
 | | Cryo-EM structure of human MLL1-NCP complex, binding mode1 | | 分子名称: | DNA (145-MER), GLUTAMINE, Histone H2A, ... | | 著者 | Huang, J, Xue, H, Yao, T. | | 登録日 | 2019-07-20 | | 公開日 | 2019-09-11 | | 最終更新日 | 2024-03-27 | | 実験手法 | ELECTRON MICROSCOPY (4.1 Å) | | 主引用文献 | Structural basis of nucleosome recognition and modification by MLL methyltransferases.
Nature, 573, 2019
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7UD5
 | | Complex between MLL1-WRAD and an H2B-ubiquitinated nucleosome | | 分子名称: | 601 DNA (146-MER), Histone H2A, Histone H2B 1.1, ... | | 著者 | Niklas, H.A, Rahman, S, Worden, E.J, Wolberger, C. | | 登録日 | 2022-03-18 | | 公開日 | 2022-09-21 | | 最終更新日 | 2022-10-05 | | 実験手法 | ELECTRON MICROSCOPY (4.25 Å) | | 主引用文献 | Multistate structures of the MLL1-WRAD complex bound to H2B-ubiquitinated nucleosome.
Proc.Natl.Acad.Sci.USA, 119, 2022
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6PWW
 | | Cryo-EM structure of MLL1 in complex with RbBP5 and WDR5 bound to the nucleosome | | 分子名称: | DNA (146-MER), Histone H2A type 1, Histone H2B 1.1, ... | | 著者 | Park, S.H, Ayoub, A, Lee, Y.T, Xu, J, Zhang, W, Zhang, B, Zhang, Y, Cianfrocco, M.A, Su, M, Dou, Y, Cho, U. | | 登録日 | 2019-07-23 | | 公開日 | 2019-12-18 | | 最終更新日 | 2024-03-20 | | 実験手法 | ELECTRON MICROSCOPY (4.4 Å) | | 主引用文献 | Cryo-EM structure of the human MLL1 core complex bound to the nucleosome.
Nat Commun, 10, 2019
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