8FXA
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![BU of 8fxa by Molmil](/molmil-images/mine/8fxa) | Bromodomain of CBP liganded with iCBP4 | 分子名称: | (6S)-1-[3,5-bis(trifluoromethyl)phenyl]-6-{(5M)-5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-[(1s,4R)-4-methoxycyclohexyl]-1H-benzimidazol-2-yl}piperidin-2-one, 1,2-ETHANEDIOL, CREB-binding protein | 著者 | Schonbrunn, E, Bikowitz, M. | 登録日 | 2023-01-24 | 公開日 | 2024-02-07 | 最終更新日 | 2024-06-05 | 実験手法 | X-RAY DIFFRACTION (1.65 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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8FXO
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![BU of 8fxo by Molmil](/molmil-images/mine/8fxo) | Bromodomain of CBP liganded with iCBP8 | 分子名称: | (6S)-1-(2,3-dihydro-1,4-benzodioxin-6-yl)-6-{(5M)-5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-[(1s,4R)-4-methoxycyclohexyl]-1H-benzimidazol-2-yl}piperidin-2-one, CREB-binding protein | 著者 | Schonbrunn, E, Bikowitz, M. | 登録日 | 2023-01-25 | 公開日 | 2024-02-07 | 最終更新日 | 2024-06-05 | 実験手法 | X-RAY DIFFRACTION (1.74 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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8G6T
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![BU of 8g6t by Molmil](/molmil-images/mine/8g6t) | Bromodomain of CBP liganded with inhibitor iCBP2 | 分子名称: | (6S)-1-(3,4-dibromophenyl)-6-{(5M)-5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-[(1s,4R)-4-methoxycyclohexyl]-1H-benzimidazol-2-yl}piperidin-2-one, CREB-binding protein, NICKEL (II) ION | 著者 | Schonbrunn, E, Bikowitz, M. | 登録日 | 2023-02-15 | 公開日 | 2024-02-21 | 最終更新日 | 2024-05-22 | 実験手法 | X-RAY DIFFRACTION (1.75 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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7JUO
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![BU of 7juo by Molmil](/molmil-images/mine/7juo) | CBP bromodomain complexed with YF2-23 | 分子名称: | CREB-binding protein, N-{1-[1,1-di(pyridin-2-yl)ethyl]-6-(1-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-3-yl)-1H-indol-4-yl}ethanesulfonamide | 著者 | Ratia, K.M, Xiong, R, Principe, D, Li, Y, Huang, F, Rana, A, Thatcher, G. | 登録日 | 2020-08-20 | 公開日 | 2021-09-01 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | 主引用文献 | XP-524 is a dual-BET/EP300 inhibitor that represses oncogenic KRAS and potentiates immune checkpoint inhibition in pancreatic cancer. Proc.Natl.Acad.Sci.USA, 119, 2022
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5KTX
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![BU of 5ktx by Molmil](/molmil-images/mine/5ktx) | CREBBP bromodomain in complex with Cpd59 ((S)-1-(3-((2-fluoro-4-(1-methyl-1H-pyrazol-4-yl)phenyl)amino)-1-(tetrahydrofuran-3-yl)-6,7-dihydro-1H-pyrazolo[4,3-c]pyridin-5(4H)-yl)ethanone) | 分子名称: | 1,2-ETHANEDIOL, 1-[3-[[2-fluoranyl-4-(1-methylpyrazol-4-yl)phenyl]amino]-1-[(3~{S})-oxolan-3-yl]-6,7-dihydro-4~{H}-pyrazolo[4,3-c]pyridin-5-yl]ethanone, CREB-binding protein, ... | 著者 | Murray, J.M, Noland, C. | 登録日 | 2016-07-12 | 公開日 | 2016-11-02 | 最終更新日 | 2024-03-06 | 実験手法 | X-RAY DIFFRACTION (1.27 Å) | 主引用文献 | Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. J. Med. Chem., 59, 2016
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5KTW
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![BU of 5ktw by Molmil](/molmil-images/mine/5ktw) | CREBBP bromodomain in complex with Cpd 44 (3-((5-acetyl-1-(cyclopropylmethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)amino)-N-isopropylbenzamide) | 分子名称: | 1,2-ETHANEDIOL, 3-[[1-(cyclopropylmethyl)-5-ethanoyl-6,7-dihydro-4~{H}-pyrazolo[4,3-c]pyridin-3-yl]amino]-~{N}-propan-2-yl-benzamide, CREB-binding protein | 著者 | Murray, J.M, Boenig, G. | 登録日 | 2016-07-12 | 公開日 | 2016-11-02 | 最終更新日 | 2024-03-06 | 実験手法 | X-RAY DIFFRACTION (1.087 Å) | 主引用文献 | Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. J. Med. Chem., 59, 2016
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5KTU
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![BU of 5ktu by Molmil](/molmil-images/mine/5ktu) | Crystal structure of the bromodomain of human CREBBP bound to pyrazolopiperidine scaffold | 分子名称: | 1-(3-phenylazanyl-1,4,6,7-tetrahydropyrazolo[4,3-c]pyridin-5-yl)ethanone, CREB-binding protein, DIMETHYL SULFOXIDE | 著者 | Jayaram, H, Poy, F, Setser, J.W, Bellon, S.F. | 登録日 | 2016-07-12 | 公開日 | 2016-11-02 | 最終更新日 | 2023-10-04 | 実験手法 | X-RAY DIFFRACTION (1.38 Å) | 主引用文献 | Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. J. Med. Chem., 59, 2016
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5NU5
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![BU of 5nu5 by Molmil](/molmil-images/mine/5nu5) | |
3I3J
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![BU of 3i3j by Molmil](/molmil-images/mine/3i3j) | Crystal Structure of the Bromodomain of Human EP300 | 分子名称: | CHLORIDE ION, DI(HYDROXYETHYL)ETHER, Histone acetyltransferase p300, ... | 著者 | Filippakopoulos, P, Picaud, S, Phillips, C, Pike, A.C.W, Muniz, J, Roos, A, Chaikuad, A, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | 登録日 | 2009-06-30 | 公開日 | 2009-07-28 | 最終更新日 | 2023-11-01 | 実験手法 | X-RAY DIFFRACTION (2.33 Å) | 主引用文献 | Histone recognition and large-scale structural analysis of the human bromodomain family. Cell(Cambridge,Mass.), 149, 2012
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5LPM
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![BU of 5lpm by Molmil](/molmil-images/mine/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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5LPK
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8FUP
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![BU of 8fup by Molmil](/molmil-images/mine/8fup) | Bromodomain of CBP liganded with BMS-536924 and CCS-1477 | 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, (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, ... | 著者 | Schonbrunn, E, Bikowitz, M. | 登録日 | 2023-01-18 | 公開日 | 2024-02-07 | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | 主引用文献 | Structural basis of CBP and EP300 interaction with kinase inhibitors To Be Published
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8FXN
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![BU of 8fxn by Molmil](/molmil-images/mine/8fxn) | Bromodomain of CBP liganded with iCBP7 | 分子名称: | 1,2-ETHANEDIOL, CREB-binding protein, tert-butyl {(1R,4s)-4-[(5M)-2-[(2S)-1-(3-tert-butylphenyl)-6-oxopiperidin-2-yl]-5-(3,5-dimethyl-1,2-oxazol-4-yl)-1H-benzimidazol-1-yl]cyclohexyl}carbamate | 著者 | Schonbrunn, E, Bikowitz, M. | 登録日 | 2023-01-25 | 公開日 | 2024-02-07 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Group 3 medulloblastoma transcriptional networks are sensitive to EP300/CBP bromodomain inhibition To be published
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7UGF
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![BU of 7ugf by Molmil](/molmil-images/mine/7ugf) | First bromodomain of BRD4 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, Bromodomain-containing protein 4 | 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 (1.45 Å) | 主引用文献 | Structural basis of CBP and EP300 interaction with kinase inhibitors To Be Published
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7UG5
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![BU of 7ug5 by Molmil](/molmil-images/mine/7ug5) | Second bromodomain of BRD3 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, Bromodomain-containing protein 3 | 著者 | Schonbrunn, E, Bikowitz, M. | 登録日 | 2022-03-23 | 公開日 | 2023-04-05 | 最終更新日 | 2023-10-25 | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | 主引用文献 | Structural basis of CBP and EP300 interaction with kinase inhibitors To Be Published
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7UGE
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![BU of 7uge by Molmil](/molmil-images/mine/7uge) | Bromodomain of CBP 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, Histone acetyltransferase | 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 (2.004 Å) | 主引用文献 | Structural basis of CBP and EP300 interaction with kinase inhibitors To Be Published
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7UGL
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![BU of 7ugl by Molmil](/molmil-images/mine/7ugl) | Bromodomain of CBP liganded with BMS-536924 and SGC-CBP30 | 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, 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 | 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 (1.5 Å) | 主引用文献 | Structural basis of CBP and EP300 interaction with kinase inhibitors To Be Published
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8E1D
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![BU of 8e1d by Molmil](/molmil-images/mine/8e1d) | |
6PF1
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6PGU
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5KJ2
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![BU of 5kj2 by Molmil](/molmil-images/mine/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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5XZC
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![BU of 5xzc by Molmil](/molmil-images/mine/5xzc) | |
3IO2
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![BU of 3io2 by Molmil](/molmil-images/mine/3io2) | Crystal structure of the Taz2 domain of p300 | 分子名称: | Histone acetyltransferase p300, SULFATE ION, ZINC ION | 著者 | Miller, M, Dauter, Z, Wlodawer, A. | 登録日 | 2009-08-13 | 公開日 | 2009-11-24 | 最終更新日 | 2024-02-21 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | Structure of the Taz2 domain of p300: insights into ligand binding. Acta Crystallogr.,Sect.D, 65, 2009
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6GYR
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![BU of 6gyr by Molmil](/molmil-images/mine/6gyr) | Transcription factor dimerization activates the p300 acetyltransferase | 分子名称: | Histone acetyltransferase p300, ZINC ION, [(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 | Panne, D, Ortega, E. | 登録日 | 2018-07-01 | 公開日 | 2018-10-17 | 最終更新日 | 2024-01-17 | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | 主引用文献 | Transcription factor dimerization activates the p300 acetyltransferase. Nature, 562, 2018
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6K4N
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![BU of 6k4n by Molmil](/molmil-images/mine/6k4n) | Cryo-EM structure of p300 | 分子名称: | Histone acetyltransferase p300 | 著者 | Ghosh, R, Roy, S, Sengupta, J. | 登録日 | 2019-05-24 | 公開日 | 2019-06-19 | 最終更新日 | 2024-03-27 | 実験手法 | ELECTRON MICROSCOPY (9.8 Å) | 主引用文献 | Tumor Suppressor p53-Mediated Structural Reorganization of the Transcriptional Coactivator p300. Biochemistry, 58, 2019
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