5BT3
| Crystal structure of EP300 bromodomain in complex with SGC-CBP30 chemical probe | 分子名称: | 2-[2-(3-chloro-4-methoxyphenyl)ethyl]-5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-[(2S)-2-(morpholin-4-yl)propyl]-1H-benzimidazole, Histone acetyltransferase p300, ISOPROPYL ALCOHOL | 著者 | Tallant, C, Hay, D, Krojer, T, Nunez-Alonso, G, Picaud, S, Newman, J.A, Fedorov, O, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Brennan, P.E, Knapp, S, Structural Genomics Consortium (SGC) | 登録日 | 2015-06-02 | 公開日 | 2015-07-01 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (1.05 Å) | 主引用文献 | Crystal structure of EP300 bromodomain in complex with a 3,5-dimethylisoxazol ligand To Be Published
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5LPM
| Crystal structure of the bromodomain of human Ep300 bound to the inhibitor XDM3d | 分子名称: | ACETATE ION, Histone acetyltransferase p300, ~{N}-[(1~{S},2~{S})-7-chloranyl-2-oxidanyl-1,2,3,4-tetrahydronaphthalen-1-yl]-4-ethanoyl-3-ethyl-5-methyl-1~{H}-pyrrole -2-carboxamide | 著者 | Huegle, M, Wohlwend, D, Gerhardt, S. | 登録日 | 2016-08-13 | 公開日 | 2017-08-16 | 最終更新日 | 2024-05-01 | 実験手法 | X-RAY DIFFRACTION (1.5 Å) | 主引用文献 | Beyond the BET Family: Targeting CBP/p300 with 4-Acyl Pyrroles. Angew. Chem. Int. Ed. Engl., 56, 2017
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3T92
| Crystal structure of the Taz2:C/EBPepsilon-TAD chimera protein | 分子名称: | 3,3',3''-phosphanetriyltripropanoic acid, ACETONE, HISTONE ACETYLTRANSFERASE P300 TAZ2-CCAAT/ENHANCER-BINDING PROTEIN EPSILON, ... | 著者 | Bhaumik, P, Maria, M. | 登録日 | 2011-08-02 | 公開日 | 2012-08-08 | 最終更新日 | 2024-02-28 | 実験手法 | X-RAY DIFFRACTION (1.5 Å) | 主引用文献 | Structural insights into interactions of C/EBP transcriptional activators with the Taz2 domain of p300. Acta Crystallogr. D Biol. Crystallogr., 70, 2014
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5NU5
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3BIY
| Crystal structure of p300 histone acetyltransferase domain in complex with a bisubstrate inhibitor, Lys-CoA | 分子名称: | BROMIDE ION, Histone acetyltransferase p300, [(2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-4-hydroxy-3-(phosphonooxy)tetrahydrofuran-2-yl]methyl (3R,20R)-20-carbamoyl-3-hydroxy-2,2-dimethyl-4,8,14,22-tetraoxo-12-thia-5,9,15,21-tetraazatricos-1-yl dihydrogen diphosphate | 著者 | Liu, X, Wang, L, Zhao, K, Thompson, P.R, Hwang, Y, Marmorstein, R, Cole, P.A. | 登録日 | 2007-12-02 | 公開日 | 2008-02-12 | 最終更新日 | 2024-02-21 | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | 主引用文献 | The structural basis of protein acetylation by the p300/CBP transcriptional coactivator Nature, 451, 2008
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6PGU
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6V8K
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4PZS
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6DS6
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5KJ2
| The novel p300/CBP inhibitor A-485 uncovers a unique mechanism of action to target AR in castrate resistant prostate cancer | 分子名称: | Histone acetyltransferase p300, N-[(4-fluorophenyl)methyl]-2-{(1R)-5-[(methylcarbamoyl)amino]-2',4'-dioxo-2,3-dihydro-3'H-spiro[indene-1,5'-[1,3]oxazolidin]-3'-yl}-N-[(2S)-1,1,1-trifluoropropan-2-yl]acetamide, SODIUM ION | 著者 | Jakob, C.G, Qiu, W, Edalji, R.P, Sun, C. | 登録日 | 2016-06-17 | 公開日 | 2017-09-27 | 最終更新日 | 2023-09-27 | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | 主引用文献 | Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours. Nature, 550, 2017
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8GZC
| Crystal structure of EP300 HAT domain in complex with compound 10 | 分子名称: | (2~{R},4~{R})-4-fluoranyl-1-[1-(4-methoxyphenyl)cyclohexyl]carbonyl-~{N}-(1~{H}-pyrazolo[4,3-b]pyridin-5-yl)pyrrolidine-2-carboxamide, Histone acetyltransferase p300, ZINC ION | 著者 | Takahashi, M, Hanzawa, H. | 登録日 | 2022-09-26 | 公開日 | 2023-01-11 | 最終更新日 | 2023-11-29 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Discovery of DS-9300: A Highly Potent, Selective, and Once-Daily Oral EP300/CBP Histone Acetyltransferase Inhibitor. J.Med.Chem., 66, 2023
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7QGS
| Crystal structure of p300 CH1 domain in complex with CITIF (a CITED2-HIF-1alpha hybrid) | 分子名称: | Cbp/p300-interacting transactivator 2,Hypoxia-inducible factor 1-alpha, Histone acetyltransferase, ZINC ION | 著者 | Hegedus, Z, Wilson, A.J, Edwards, T.A. | 登録日 | 2021-12-10 | 公開日 | 2022-05-11 | 最終更新日 | 2024-01-31 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Understanding p300-transcription factor interactions using sequence variation and hybridization. Rsc Chem Biol, 3, 2022
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7UGI
| Bromodomain of EP300 liganded with BMS-536924 | 分子名称: | (3M)-4-{[(2S)-2-(3-chlorophenyl)-2-hydroxyethyl]amino}-3-[4-methyl-6-(morpholin-4-yl)-1H-benzimidazol-2-yl]pyridin-2(1H)-one, 1,2-ETHANEDIOL, 3,6,9,12,15,18,21,24-OCTAOXAHEXACOSAN-1-OL, ... | 著者 | Schonbrunn, E, Bikowitz, M. | 登録日 | 2022-03-24 | 公開日 | 2023-04-12 | 最終更新日 | 2023-10-25 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Structural basis of CBP and EP300 interaction with kinase inhibitors To Be Published
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7VHZ
| Crystal structure of EP300 HAT domain in complex with compound 7 | 分子名称: | (2R)-N-(2H-indazol-4-yl)-1-[1-(4-methoxyphenyl)cyclopentyl]carbonyl-pyrrolidine-2-carboxamide, Histone acetyltransferase p300, ZINC ION | 著者 | Takahashi, M, Hanzawa, H. | 登録日 | 2021-09-24 | 公開日 | 2022-04-27 | 最終更新日 | 2023-11-29 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Discovery of EP300/CBP histone acetyltransferase inhibitors through scaffold hopping of 1,4-oxazepane ring. Bioorg.Med.Chem.Lett., 66, 2022
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5LKT
| Crystal structure of the p300 acetyltransferase catalytic core with butyryl-coenzyme A. | 分子名称: | Butyryl Coenzyme A, CHLORIDE ION, DIMETHYL SULFOXIDE, ... | 著者 | Kaczmarska, Z, Ortega, E, Marquez, J.A, Panne, D. | 登録日 | 2016-07-24 | 公開日 | 2016-11-02 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (2.04 Å) | 主引用文献 | Structure of p300 in complex with acyl-CoA variants. Nat. Chem. Biol., 13, 2017
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6V90
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4PZR
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5LPK
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8FVF
| Bromodomain of EP300 liganded with CCS-1477 | 分子名称: | (6S)-1-[3,4-bis(fluoranyl)phenyl]-6-[5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-(4-methoxycyclohexyl)benzimidazol-2-yl]piperidin-2-one, 1,2-ETHANEDIOL, Histone acetyltransferase p300, ... | 著者 | Schonbrunn, E, Bikowitz, M. | 登録日 | 2023-01-18 | 公開日 | 2024-02-07 | 最終更新日 | 2024-06-05 | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | 主引用文献 | Group 3 medulloblastoma transcriptional networks collapse under domain specific EP300/CBP inhibition. Nat Commun, 15, 2024
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7VI0
| Crystal structure of EP300 HAT domain in complex with compound 11 | 分子名称: | (4S)-N-(3H-indazol-4-yl)-3-[1-(4-methoxyphenyl)cyclopentyl]carbonyl-1,1-bis(oxidanylidene)-1,3-thiazolidine-4-carboxamide, Histone acetyltransferase p300, ZINC ION | 著者 | Takahashi, M, Hanzawa, H. | 登録日 | 2021-09-24 | 公開日 | 2022-04-27 | 最終更新日 | 2023-11-29 | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | 主引用文献 | Discovery of EP300/CBP histone acetyltransferase inhibitors through scaffold hopping of 1,4-oxazepane ring. Bioorg.Med.Chem.Lett., 66, 2022
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7SS8
| Human P300 complexed with a proline-based inhibitor | 分子名称: | 1,2-ETHANEDIOL, 1-[1-(4-chlorophenyl)cyclopentane-1-carbonyl]-N-{[3-(methylcarbamoyl)phenyl]methyl}-D-prolinamide, Histone acetyltransferase p300, ... | 著者 | Shewchuk, L.M, Reid, R.A. | 登録日 | 2021-11-10 | 公開日 | 2022-11-09 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (2.15 Å) | 主引用文献 | Discovery of Proline-Based p300/CBP Inhibitors Using DNA-Encoded Library Technology in Combination with High-Throughput Screening. J.Med.Chem., 65, 2022
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3P57
| Crystal structure of the p300 TAZ2 domain bound to MEF2 on DNA | 分子名称: | DNA (5'-D(*A*AP*AP*CP*TP*AP*TP*TP*TP*AP*TP*AP*AP*GP*A)-3'), DNA (5'-D(*TP*TP*CP*TP*TP*AP*TP*AP*AP*AP*TP*AP*GP*TP*T)-3'), Histone acetyltransferase p300, ... | 著者 | He, J, Ye, J, Riquelme, C, Liu, J.O. | 登録日 | 2010-10-08 | 公開日 | 2011-08-10 | 最終更新日 | 2023-09-06 | 実験手法 | X-RAY DIFFRACTION (2.1921 Å) | 主引用文献 | Structure of p300 bound to MEF2 on DNA reveals a mechanism of enhanceosome assembly. Nucleic Acids Res., 39, 2011
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6V8N
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7VHY
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6PF1
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