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
|
|
6N31
 | | WD repeats of human WDR12 | | 分子名称: | Ribosome biogenesis protein WDR12, UNKNOWN ATOM OR ION | | 著者 | Halabelian, L, Zeng, H, Tempel, W, Li, Y, Seitova, A, Hutchinson, A, Bountra, C, Edwards, A.M, Arrowsmith, C.H, Structural Genomics Consortium (SGC) | | 登録日 | 2018-11-14 | | 公開日 | 2018-12-12 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | WD repeats of human WDR12
To Be Published
|
|
6OI0
 | | 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
|
|
5H13
 | | EED in complex with PRC2 allosteric inhibitor EED396 | | 分子名称: | 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, ... | | 著者 | Zhao, K, Zhao, M, Luo, X, Zhang, H. | | 登録日 | 2016-10-08 | | 公開日 | 2017-01-25 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED
PLoS ONE, 12, 2017
|
|
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
|
|
5KWN
 | |
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
|
|
5M23
 | | 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
|
|
5MWJ
 | | Structure Enabled Discovery of a Stapled Peptide Inhibitor to Target the Oncogenic Transcriptional Repressor TLE1 | | 分子名称: | DIMETHYL SULFOXIDE, Transducin-like enhancer protein 1, pepide inhibtor | | 著者 | McGrath, S, Tortorici, M, Vidler, L, Drouin, L, Westwood, I, Gimeson, P, Van Montfort, R, Hoelder, S. | | 登録日 | 2017-01-18 | | 公開日 | 2017-04-05 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.04 Å) | | 主引用文献 | Structure-Enabled Discovery of a Stapled Peptide Inhibitor to Target the Oncogenic Transcriptional Repressor TLE1.
Chemistry, 23, 2017
|
|
5N4A
 | | Crystal structure of Chlamydomonas IFT80 | | 分子名称: | GLYCEROL, Intraflagellar transport protein 80, OXALATE ION | | 著者 | Taschner, M, Mourao, A. | | 登録日 | 2017-02-10 | | 公開日 | 2018-02-28 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (1.79 Å) | | 主引用文献 | Crystal structure of intraflagellar transport protein 80 reveals a homo-dimer required for ciliogenesis.
Elife, 7, 2018
|
|
5M89
 | | Spliceosome component | | 分子名称: | Spliceosome WD40 Sc | | 著者 | Moura, T.R, Pena, V. | | 登録日 | 2016-10-28 | | 公開日 | 2018-03-14 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.605 Å) | | 主引用文献 | Prp19/Pso4 Is an Autoinhibited Ubiquitin Ligase Activated by Stepwise Assembly of Three Splicing Factors.
Mol. Cell, 69, 2018
|
|
5MZH
 | | Crystal structure of ODA16 from Chlamydomonas reinhardtii | | 分子名称: | Dynein assembly factor with WDR repeat domains 1, SULFATE ION | | 著者 | Lorentzen, E, Taschner, M, Basquin, J, Mourao, A. | | 登録日 | 2017-01-31 | | 公開日 | 2017-03-22 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.398 Å) | | 主引用文献 | Structural basis of outer dynein arm intraflagellar transport by the transport adaptor protein ODA16 and the intraflagellar transport protein IFT46.
J. Biol. Chem., 292, 2017
|
|
5N1A
 | |
5M2N
 | |
5NAF
 | |
5NNZ
 | | Crystal structure of human ODA16 | | 分子名称: | Dynein assembly factor with WDR repeat domains 1 | | 著者 | Lorentzen, E, Taschner, T, Basquin, J. | | 登録日 | 2017-04-10 | | 公開日 | 2017-06-07 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (2.651 Å) | | 主引用文献 | Purification and crystal structure of human ODA16: Implications for ciliary import of outer dynein arms by the intraflagellar transport machinery.
Protein Sci., 29, 2020
|
|
6UOZ
 | |
6V3X
 | |
6V3Y
 | |
6W7G
 | | Structure of EED bound to inhibitor 1056 | | 分子名称: | 8-(2,6-dimethylpyridin-3-yl)-N-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methyl]-1-(methylsulfonyl)imidazo[1,5-c]pyrimidin-5-amine, FORMIC ACID, Polycomb protein EED, ... | | 著者 | Petrunak, E.M, Stuckey, J.A. | | 登録日 | 2020-03-19 | | 公開日 | 2020-07-08 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | | 主引用文献 | EEDi-5285: An Exceptionally Potent, Efficacious, and Orally Active Small-Molecule Inhibitor of Embryonic Ectoderm Development.
J.Med.Chem., 63, 2020
|
|
6WJQ
 | |
6VYC
 | | Crystal structure of WD-repeat domain of human WDR91 | | 分子名称: | UNKNOWN ATOM OR ION, WD repeat-containing protein 91 | | 著者 | Halabelian, L, Hutchinson, A, Li, Y, Seitova, A, Bountra, C, Edwards, A.M, Arrowsmith, C.H, Structural Genomics Consortium (SGC) | | 登録日 | 2020-02-26 | | 公開日 | 2020-03-25 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Discovery of a First-in-Class Small-Molecule Ligand for WDR91 Using DNA-Encoded Chemical Library Selection Followed by Machine Learning.
J.Med.Chem., 66, 2023
|
|
6W7F
 | | Structure of EED bound to inhibitor 5285 | | 分子名称: | 8-(6-cyclopropylpyridin-3-yl)-N-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methyl]-1-(methylsulfonyl)imidazo[1,5-c]pyrimidin-5-amine, GLYCEROL, Polycomb protein EED | | 著者 | Petrunak, E.M, Stuckey, J.A. | | 登録日 | 2020-03-19 | | 公開日 | 2020-07-08 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | EEDi-5285: An Exceptionally Potent, Efficacious, and Orally Active Small-Molecule Inhibitor of Embryonic Ectoderm Development.
J.Med.Chem., 63, 2020
|
|
7P3J
 | | EED in complex with compound 4 | | 分子名称: | 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, ... | | 著者 | Read, J.A. | | 登録日 | 2021-07-07 | | 公開日 | 2021-12-08 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (1.93 Å) | | 主引用文献 | Diverse, Potent, and Efficacious Inhibitors That Target the EED Subunit of the Polycomb Repressive Complex 2 Methyltransferase.
J.Med.Chem., 64, 2021
|
|
7P3C
 | | EED in complex with compound 4 | | 分子名称: | 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 | | 著者 | Read, J.A. | | 登録日 | 2021-07-07 | | 公開日 | 2021-12-08 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (1.61 Å) | | 主引用文献 | Diverse, Potent, and Efficacious Inhibitors That Target the EED Subunit of the Polycomb Repressive Complex 2 Methyltransferase.
J.Med.Chem., 64, 2021
|
|
