8SDX
 
 | | ATAD2B bromodomain in complex with histone H4 acetylated at lysine 5 with Serine 1 mutation to Cysteine | | Descriptor: | ATPase family AAA domain-containing protein 2B, SULFATE ION, histone H4S1CK5ac | | Authors: | Phillips, M, Montgomery, C, Nix, J.C, Glass, K.C. | | Deposit date: | 2023-04-07 | | Release date: | 2024-06-05 | | Method: | X-RAY DIFFRACTION (2.69 Å) | | Cite: | Impact of Combinatorial Histone Modifications on Acetyllysine Recognition by the ATAD2 and ATAD2B Bromodomains.
J.Med.Chem., 67, 2024
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2R0S
 | | Crystal Structure of the Rsc4 tandem bromodomain | | Descriptor: | Chromatin structure-remodeling complex protein RSC4 | | Authors: | VanDemark, A.P, Kasten, M.M, Ferris, E, Heroux, A, Hill, C.P, Cairns, B.R. | | Deposit date: | 2007-08-21 | | Release date: | 2007-10-30 | | Last modified: | 2017-10-25 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Autoregulation of the rsc4 tandem bromodomain by gcn5 acetylation.
Mol.Cell, 27, 2007
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6DF4
 | | TAF1-BD2 in complex with Cpd8 (6-(but-3-en-1-yl)-4-(3-(morpholine-4-carbonyl)phenyl)-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one) | | Descriptor: | 6-(but-3-en-1-yl)-4-[3-(morpholine-4-carbonyl)phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one, Transcription initiation factor TFIID subunit | | Authors: | Murray, J.M, Tang, Y. | | Deposit date: | 2018-05-14 | | Release date: | 2018-10-31 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (1.3 Å) | | Cite: | GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like.
J. Med. Chem., 61, 2018
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6DF7
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6DDI
 | | Crystal Structure of the human BRD2 BD1 bromodomain in complex with a Tetrahydroquinoline analogue | | Descriptor: | 1,2-ETHANEDIOL, 4-{[(2S,4R)-1-acetyl-2-methyl-6-(1H-pyrazol-3-yl)-1,2,3,4-tetrahydroquinolin-4-yl]amino}benzonitrile, Bromodomain-containing protein 2, ... | | Authors: | White, S.W, Yun, M. | | Deposit date: | 2018-05-10 | | Release date: | 2019-11-13 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | Bromodomain-Selective BET Inhibitors Are Potent Antitumor Agents against MYC-Driven Pediatric Cancer.
Cancer Res., 80, 2020
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2YQD
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6DML
 | | A multiconformer ligand model of 3,5 dimethylisoxaxole bound to the bromodomain of human BRD4 | | Descriptor: | 1,2-ETHANEDIOL, 4-((2-(tert-butyl)phenyl)amino)-7-(3,5-dimethylisoxazol-4-yl)-6-methoxy-1,5-naphthyridine-3-carboxylic acid, Bromodomain-containing protein 4 | | Authors: | Hudson, B.M, van Zundert, G, Keedy, D.A, Fonseca, R, Heliou, A, Suresh, P, Borrelli, K, Day, T, Fraser, J.S, van den Bedem, H. | | Deposit date: | 2018-06-05 | | Release date: | 2018-12-19 | | Last modified: | 2024-05-01 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | qFit-ligand Reveals Widespread Conformational Heterogeneity of Drug-Like Molecules in X-Ray Electron Density Maps.
J. Med. Chem., 61, 2018
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2RFJ
 | | Crystal structure of the bromo domain 1 in human bromodomain containing protein, testis specific (BRDT) | | Descriptor: | Bromodomain testis-specific protein | | Authors: | Filippakopoulos, P, Salah, E, Savitsky, P, Keates, T, Parizotto, E, Elkins, J, Pike, A.C.W, Ugochukwu, E, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Sundstrom, M, Knapp, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2007-09-30 | | Release date: | 2007-10-23 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.05 Å) | | Cite: | Histone recognition and large-scale structural analysis of the human bromodomain family.
Cell(Cambridge,Mass.), 149, 2012
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2MJV
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6DB0
 | | N-Terminal bromodomain of Human BRD2 with a Tetrahydroquinoline analogue | | Descriptor: | 1,2-ETHANEDIOL, 1-[(2S,4R)-4-[(2-chlorophenyl)amino]-2-methyl-6-(1H-pyrazol-3-yl)-3,4-dihydroquinolin-1(2H)-yl]ethan-1-one, 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, ... | | Authors: | White, S.W, Yun, M. | | Deposit date: | 2018-05-02 | | Release date: | 2019-11-13 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | N-Terminal bromodomain of Human BRD2 with a Tetrahydroquinoline analogue
To Be Published
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6DBC
 | | Second bromodomain of Human BRD2 with a Tetrahydroquinoline analogue | | Descriptor: | 1,2-ETHANEDIOL, 1-[(2S,4R)-4-[(2-chlorophenyl)amino]-2-methyl-6-(1H-pyrazol-3-yl)-3,4-dihydroquinolin-1(2H)-yl]ethan-1-one, Bromodomain-containing protein 2 | | Authors: | White, S.W, Yun, M. | | Deposit date: | 2018-05-03 | | Release date: | 2019-11-13 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (1.05 Å) | | Cite: | Second bromodomain of Human BRD2 with a Tetrahydroquinoline analogue
To Be Published
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6DNE
 | | Crystal structure of human Bromodomain-containing protein 4 (BRD4) bromodomain with MS660 | | Descriptor: | Bromodomain-containing protein 4, N,N'-[ethane-1,2-diylbis(oxyethane-2,1-diyl)]bis{2-[(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetamide} | | Authors: | Ren, C, Zhou, M.M. | | Deposit date: | 2018-06-06 | | Release date: | 2018-07-18 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.958 Å) | | Cite: | Spatially constrained tandem bromodomain inhibition bolsters sustained repression of BRD4 transcriptional activity for TNBC cell growth.
Proc. Natl. Acad. Sci. U.S.A., 115, 2018
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6DMJ
 | | A multiconformer ligand model of inhibitor 53W bound to CREB binding protein bromodomain | | Descriptor: | 5-(3,5-dimethyl-1,2-oxazol-4-yl)-2-[2-(4-methoxyphenyl)ethyl]-1-[2-(morpholin-4-yl)ethyl]-1H-benzimidazole, Bromodomain-containing protein 4 | | Authors: | Hudson, B.M, van Zundert, G, Keedy, D.A, Fonseca, R, Heliou, A, Suresh, P, Borrelli, K, Day, T, Fraser, J.S, van den Bedem, H. | | Deposit date: | 2018-06-05 | | Release date: | 2018-12-19 | | Last modified: | 2024-05-01 | | Method: | X-RAY DIFFRACTION (1.15 Å) | | Cite: | qFit-ligand Reveals Widespread Conformational Heterogeneity of Drug-Like Molecules in X-Ray Electron Density Maps.
J. Med. Chem., 61, 2018
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6DDJ
 | | Crystal Structure of the human BRD2 BD2 bromodimain in complex with a Tetrahydroquinoline analogue | | Descriptor: | 1,2-ETHANEDIOL, 4-{[(2S,4R)-1-acetyl-2-methyl-6-(1H-pyrazol-3-yl)-1,2,3,4-tetrahydroquinolin-4-yl]amino}benzonitrile, Bromodomain-containing protein 2 | | Authors: | White, S.W, Yun, M. | | Deposit date: | 2018-05-10 | | Release date: | 2019-11-13 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (1.05 Å) | | Cite: | Bromodomain-Selective BET Inhibitors Are Potent Antitumor Agents against MYC-Driven Pediatric Cancer.
Cancer Res., 80, 2020
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2RNW
 | | The Structural Basis for Site-Specific Lysine-Acetylated Histone Recognition by the Bromodomains of the Human Transcriptional Co-Activators PCAf and CBP | | Descriptor: | Histone H3, Histone acetyltransferase PCAF | | Authors: | Zeng, L, Zhang, Q, Gerona-Navarro, G, Zhou, M.M. | | Deposit date: | 2008-02-03 | | Release date: | 2008-05-06 | | Last modified: | 2023-11-15 | | Method: | SOLUTION NMR | | Cite: | Structural Basis of Site-Specific Histone Recognition by the Bromodomains of Human Coactivators PCAF and CBP/p300
Structure, 16, 2008
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2RNX
 | | The Structural Basis for Site-Specific Lysine-Acetylated Histone Recognition by the Bromodomains of the HUman Transcriptional Co-Activators PCAF and CBP | | Descriptor: | Histone H3, Histone acetyltransferase PCAF | | Authors: | Zeng, L, Zhang, Q, Gerona-Navarro, G, Zhou, M.M. | | Deposit date: | 2008-02-03 | | Release date: | 2008-05-06 | | Last modified: | 2023-11-15 | | Method: | SOLUTION NMR | | Cite: | Structural Basis of Site-Specific Histone Recognition by the Bromodomains of Human Coactivators PCAF and CBP/p300
Structure, 16, 2008
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2RNY
 | | Complex Structures of CBP Bromodomain with H4 ack20 Peptide | | Descriptor: | CREB-binding protein, Histone H4 | | Authors: | Zeng, L, Zhang, Q, Gerona-Navarro, G, Zhou, M.M. | | Deposit date: | 2008-02-03 | | Release date: | 2008-05-06 | | Last modified: | 2023-11-15 | | Method: | SOLUTION NMR | | Cite: | Structural Basis of Site-Specific Histone Recognition by the Bromodomains of Human Coactivators PCAF and CBP/p300
Structure, 16, 2008
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2RS9
 | | Solution structure of the bromodomain of human BRPF1 in complex with histone H4K5ac peptide | | Descriptor: | Acetylated lysine 5 of peptide from Histone H4, Peregrin | | Authors: | Qin, X, Nagashima, T, Umehara, T, Hayashi, F, Yokoyama, S, RIKEN Structural Genomics/Proteomics Initiative (RSGI) | | Deposit date: | 2011-12-08 | | Release date: | 2012-12-12 | | Last modified: | 2023-11-15 | | Method: | SOLUTION NMR | | Cite: | Site-specific histone recognition by the bromodomain of Brpf1 and the role in MOZ/MORF histone acetyltransferase complexes
To be Published
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2YEM
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2YDW
 | | Crystal Structure of the First Bromodomain of Human Brd2 with the inhibitor GW841819X | | Descriptor: | BENZYL [(4R)-1-METHYL-6-PHENYL-4H-[1,2,4]TRIAZOLO[4,3-A][1,4]BENZODIAZEPIN-4-YL]CARBAMATE, BROMODOMAIN-CONTAINING PROTEIN 2, SULFATE ION | | Authors: | Chung, C, Delves, C, Woodward, R, Mirguet, O, Nicodeme, E. | | Deposit date: | 2011-03-24 | | Release date: | 2011-06-15 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Discovery and Characterization of Small Molecule Inhibitors of the Bet Family Bromodomains.
J.Med.Chem., 54, 2011
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2I7K
 | | Solution Structure of the Bromodomain of Human BRD7 Protein | | Descriptor: | Bromodomain-containing protein 7 | | Authors: | Sun, H, Liu, J, Zhang, J, Huang, H, Wu, J, Shi, Y. | | Deposit date: | 2006-08-31 | | Release date: | 2007-07-10 | | Last modified: | 2024-05-29 | | Method: | SOLUTION NMR | | Cite: | Solution structure of BRD7 bromodomain and its interaction with acetylated peptides from histone H3 and H4
Biochem.Biophys.Res.Commun., 358, 2007
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2YEK
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2WP2
 | | Structure of Brdt bromodomain BD1 bound to a diacetylated histone H4 peptide. | | Descriptor: | BROMODOMAIN TESTIS-SPECIFIC PROTEIN, HISTONE H4 | | Authors: | Moriniere, J, Rousseaux, S, Steuerwald, U, Soler-Lopez, M, Curtet, S, Vitte, A.-L, Govin, J, Gaucher, J, Sadoul, K, Hart, D.J, Krijgsveld, J, Khochbin, S, Mueller, C.W, Petosa, C. | | Deposit date: | 2009-08-02 | | Release date: | 2009-09-22 | | Last modified: | 2024-05-01 | | Method: | X-RAY DIFFRACTION (2.37 Å) | | Cite: | Cooperative Binding of Two Acetylation Marks on a Histone Tail by a Single Bromodomain.
Nature, 461, 2009
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2YW5
 | | Solution structure of the bromodomain from human bromodomain containing protein 3 | | Descriptor: | Bromodomain-containing protein 3 | | Authors: | Furue, M, Suzuki, S, Muto, Y, Inoue, M, Kigawa, T, Terada, T, Shirouzu, M, Yokoyama, S, RIKEN Structural Genomics/Proteomics Initiative (RSGI) | | Deposit date: | 2007-04-19 | | Release date: | 2008-04-22 | | Last modified: | 2024-05-29 | | Method: | SOLUTION NMR | | Cite: | Solution structure of the bromodomain from human bromodomain containing protein 3
To be Published
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2YEL
 | | Crystal Structure of the First Bromodomain of Human Brd4 with the inhibitor GW841819X | | Descriptor: | 1,2-ETHANEDIOL, BENZYL [(4R)-1-METHYL-6-PHENYL-4H-[1,2,4]TRIAZOLO[4,3-A][1,4]BENZODIAZEPIN-4-YL]CARBAMATE, HUMAN BRD4 | | Authors: | Chung, C.W. | | Deposit date: | 2011-03-25 | | Release date: | 2011-06-15 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (1.65 Å) | | Cite: | Discovery and Characterization of Small Molecule Inhibitors of the Bet Family Bromodomains.
J.Med.Chem., 54, 2011
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