7EGJ
 
 | | SCP promoter-bound TFIID-TFIIA in post TBP-loading state | | Descriptor: | DNA (74-MER), TATA-box-binding protein, Transcription initiation factor IIA subunit 1, ... | | Authors: | Chen, X, Wu, Z, Li, J, Zhao, D, Xu, Y. | | Deposit date: | 2021-03-24 | | Release date: | 2021-05-12 | | Method: | ELECTRON MICROSCOPY (8.64 Å) | | Cite: | Structural insights into preinitiation complex assembly on core promoters.
Science, 372, 2021
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7EGE
 | | TFIID in canonical conformation | | Descriptor: | TATA-box-binding protein, Transcription initiation factor TFIID subunit 1, Transcription initiation factor TFIID subunit 10, ... | | Authors: | Chen, X, Wu, Z, Li, J, Zhao, D, Xu, Y. | | Deposit date: | 2021-03-24 | | Release date: | 2021-05-12 | | Method: | ELECTRON MICROSCOPY (9 Å) | | Cite: | Structural insights into preinitiation complex assembly on core promoters.
Science, 372, 2021
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7EGC
 | | p53-bound TFIID-based holo PIC on HDM2 promoter | | Descriptor: | CDK-activating kinase assembly factor MAT1, Cyclin-H, Cyclin-dependent kinase 7, ... | | Authors: | Chen, X, Wu, Z, Hou, H, Qi, Y, Wang, X, Li, J, Xu, Y. | | Deposit date: | 2021-03-24 | | Release date: | 2021-05-12 | | Method: | ELECTRON MICROSCOPY (3.9 Å) | | Cite: | Structural insights into preinitiation complex assembly on core promoters.
Science, 372, 2021
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7EDX
 | | p53-bound TFIID-based core PIC on HDM2 promoter | | Descriptor: | DNA (84-mer), DNA-directed RNA polymerase II subunit E, DNA-directed RNA polymerase II subunit F, ... | | Authors: | Chen, X, Qi, Y, Hou, H, Wang, X, Wu, Z, Li, J, Xu, Y. | | Deposit date: | 2021-03-17 | | Release date: | 2021-05-05 | | Last modified: | 2021-05-19 | | Method: | ELECTRON MICROSCOPY (4.5 Å) | | Cite: | Structural insights into preinitiation complex assembly on core promoters.
Science, 372, 2021
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7M2E
 | | Crystal structure of BPTF bromodomain in complex with CB02-092 | | Descriptor: | 4-chloro-5-{4-[2-(dimethylamino)ethyl]anilino}-2-methylpyridazin-3(2H)-one, Nucleosome-remodeling factor subunit BPTF | | Authors: | Nithianantham, S, Fischer, M. | | Deposit date: | 2021-03-16 | | Release date: | 2022-02-16 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.75 Å) | | Cite: | New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition
J.Med.Chem., 64, 2021
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7M16
 | | Triazole-based BET family bromodomain inhibitor bound to BRD4(D1) | | Descriptor: | 4-{5-[6-(3,5-dimethylanilino)pyridin-2-yl]-4-methyl-1H-1,2,3-triazol-1-yl}piperidine-1-carboximidamide, Bromodomain-containing protein 4 | | Authors: | Johnson, J.A, Pomerantz, W. | | Deposit date: | 2021-03-12 | | Release date: | 2021-09-29 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.42 Å) | | Cite: | Systematically Mitigating the p38alpha Activity of Triazole-based BET Inhibitors
ACS Med. Chem. Lett., 10, 2019
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7EBK
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7EBJ
 | | Apo structure of the mouse Trim66 PHD-Bromo dual domain | | Descriptor: | Tripartite motif-containing protein 66, ZINC ION | | Authors: | Wang, Z, Jiang, J. | | Deposit date: | 2021-03-09 | | Release date: | 2022-03-09 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | A TRIM66/DAX1/Dux axis suppresses the totipotent 2-cell-like state in murine embryonic stem cells.
Cell Stem Cell, 29, 2022
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7NQ5
 | | C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH 3-(2-(benzyloxy)phenyl)-5-methyl-1H-1,2,4-triazole | | Descriptor: | 1,2-ETHANEDIOL, 2-{2-[2-(2-{2-[2-(2-ETHOXY-ETHOXY)-ETHOXY]-ETHOXY}-ETHOXY)-ETHOXY]-ETHOXY}-ETHANOL, 3-methyl-5-(2-phenylmethoxyphenyl)-4~{H}-1,2,4-triazole, ... | | Authors: | Chung, C. | | Deposit date: | 2021-03-01 | | Release date: | 2021-03-24 | | Last modified: | 2021-04-07 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
J.Med.Chem., 64, 2021
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7NQ8
 | | C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH N-ethyl-3-(1-methyl-1H-1,2,3-triazol-4-yl)-4-(pyridin-2-ylmethoxy)benzamide | | Descriptor: | 1,2-ETHANEDIOL, Bromodomain-containing protein 2, N-ethyl-3-(1-methyl-1H-1,2,3-triazol-4-yl)-4-(pyridin-2-ylmethoxy)benzamide | | Authors: | Chung, C.W. | | Deposit date: | 2021-03-01 | | Release date: | 2021-03-24 | | Last modified: | 2021-04-07 | | Method: | X-RAY DIFFRACTION (1.602 Å) | | Cite: | Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
J.Med.Chem., 64, 2021
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7NQI
 | | C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH 2-benzyl-N-cyclopropyl-6-(1-methyl-1H-1,2,3-triazol-4-yl)isonicotinamide | | Descriptor: | 1,2-ETHANEDIOL, 2-benzyl-N-cyclopropyl-6-(1-methyl-1H-1,2,3-triazol-4-yl)isonicotinamide, Bromodomain-containing protein 2 | | Authors: | Chung, C.W. | | Deposit date: | 2021-03-01 | | Release date: | 2021-03-24 | | Last modified: | 2021-04-07 | | Method: | X-RAY DIFFRACTION (1.603 Å) | | Cite: | Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
J.Med.Chem., 64, 2021
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7NQ9
 | | C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH 2-benzyl-N-cyclopropyl-6-(1-methyl-1H-1,2,3-triazol-4-yl)isonicotinamide | | Descriptor: | 1,2-ETHANEDIOL, 6-benzyl-N4-((1r,3r)-3-hydroxycyclobutyl)-N2-methylpyridine-2,4-dicarboxamide, Bromodomain-containing protein 2 | | Authors: | Chung, C.W. | | Deposit date: | 2021-03-01 | | Release date: | 2021-03-24 | | Last modified: | 2021-04-07 | | Method: | X-RAY DIFFRACTION (1.602 Å) | | Cite: | Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
J.Med.Chem., 64, 2021
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7NQ7
 | | C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH (S)-N-ethyl-3-(1-methyl-1H-1,2,3-triazol-4-yl)-4-(1-phenylethoxy)benzamide | | Descriptor: | 1,2-ETHANEDIOL, Bromodomain-containing protein 2, ~{N}-ethyl-3-(1-methyl-1,2,3-triazol-4-yl)-4-[(1~{S})-1-phenylethoxy]benzamide | | Authors: | Chung, C. | | Deposit date: | 2021-03-01 | | Release date: | 2021-03-24 | | Last modified: | 2021-04-07 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
J.Med.Chem., 64, 2021
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7NQJ
 | | C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH N-ethyl-2-(1-methyl-1H-1,2,3-triazol-4-yl)-6-(1-phenylethyl)isonicotinamide | | Descriptor: | 1,2-ETHANEDIOL, Bromodomain-containing protein 2, DI(HYDROXYETHYL)ETHER, ... | | Authors: | Chung, C. | | Deposit date: | 2021-03-01 | | Release date: | 2021-04-07 | | Method: | X-RAY DIFFRACTION (1.734 Å) | | Cite: | Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
J.Med.Chem., 64, 2021
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7NQ1
 | | C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH 6-((S)-hydroxy(phenyl)methyl)-N2-methyl-N4-((1S,2S)-2-methylcyclopropyl)pyridine-2,4-dicarboxamide | | Descriptor: | 1,2-ETHANEDIOL, Bromodomain-containing protein 2, ~{N}2-methyl-~{N}4-[(1~{S},2~{S})-2-methylcyclopropyl]-6-[(~{S})-oxidanyl(phenyl)methyl]pyridine-2,4-dicarboxamide | | Authors: | Chung, C. | | Deposit date: | 2021-02-28 | | Release date: | 2021-07-21 | | Last modified: | 2021-08-25 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | Identification of a Series of N -Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins.
J.Med.Chem., 64, 2021
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7NPY
 | | C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH 6-benzyl-N2-methyl-N4-((1S,2S)-2-methylcyclopropyl)pyridine-2,4-dicarboxamide | | Descriptor: | 1,2-ETHANEDIOL, Bromodomain-containing protein 2, ~{N}2-methyl-~{N}4-[(1~{S},2~{S})-2-methylcyclopropyl]-6-(phenylmethyl)pyridine-2,4-dicarboxamide | | Authors: | Chung, C. | | Deposit date: | 2021-02-28 | | Release date: | 2021-07-21 | | Last modified: | 2021-08-25 | | Method: | X-RAY DIFFRACTION (1.601 Å) | | Cite: | Identification of a Series of N -Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins.
J.Med.Chem., 64, 2021
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7NQ2
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7NPZ
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7NQ0
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7NQ3
 | | C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH N4-((1R,5S,6r)-3-oxabicyclo[3.1.0]hexan-6-yl)-6-((S)-methoxy(phenyl)methyl)-N2-methylpyridine-2,4-dicarboxamide | | Descriptor: | 1,2-ETHANEDIOL, 6-[(~{S})-methoxy(phenyl)methyl]-~{N}2-methyl-~{N}4-[(1~{S},5~{R})-3-oxabicyclo[3.1.0]hexan-6-yl]pyridine-2,4-dicarboxamide, Bromodomain-containing protein 2 | | Authors: | Chung, C. | | Deposit date: | 2021-02-28 | | Release date: | 2021-07-21 | | Last modified: | 2021-08-25 | | Method: | X-RAY DIFFRACTION (1.603 Å) | | Cite: | Identification of a Series of N -Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins.
J.Med.Chem., 64, 2021
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7LRO
 | | Crystal structure of BPTF bromodomain in complex with inhibitor HZ-01-105 | | Descriptor: | 1,2-ETHANEDIOL, 5-(azetidin-3-ylamino)-4-chloranyl-2-methyl-pyridazin-3-one, DIMETHYL SULFOXIDE, ... | | Authors: | Chan, A, Schonbrunn, E. | | Deposit date: | 2021-02-17 | | Release date: | 2022-08-10 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (1.45 Å) | | Cite: | New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition.
J.Med.Chem., 64, 2021
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7LRK
 | | Crystal structure of BPTF bromodomain in complex with inhibitor Pdy-3-093 | | Descriptor: | 1,2-ETHANEDIOL, 4-chloranyl-2-methyl-5-[[(3~{S})-pyrrolidin-3-yl]amino]pyridazin-3-one, Nucleosome-remodeling factor subunit BPTF | | Authors: | Chan, A, Schonbrunn, E. | | Deposit date: | 2021-02-16 | | Release date: | 2022-08-10 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (1.44 Å) | | Cite: | New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition.
J.Med.Chem., 64, 2021
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7LPK
 | | Crystal structure of BPTF bromodomain in complex with inhibitor HZ-03-112 | | Descriptor: | 1,2-ETHANEDIOL, 4-chloranyl-2-methyl-5-[[(3~{R})-pyrrolidin-3-yl]amino]pyridazin-3-one, Nucleosome-remodeling factor subunit BPTF | | Authors: | Chan, A, Schonbrunn, E. | | Deposit date: | 2021-02-12 | | Release date: | 2022-08-10 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (1.39 Å) | | Cite: | New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition.
J.Med.Chem., 64, 2021
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7LP0
 | | Crystal structure of BPTF bromodomain in complex with inhibitor Pdy-3-077 | | Descriptor: | 1,2-ETHANEDIOL, 4-chlorol-2-methyl-5-[[(3~{R})-1-methylpiperidin-3-yl]amino]pyridazin-3-one, DIMETHYL SULFOXIDE, ... | | Authors: | Chan, A, Schonbrunn, E. | | Deposit date: | 2021-02-11 | | Release date: | 2022-08-10 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (1.66 Å) | | Cite: | New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition.
J.Med.Chem., 64, 2021
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7LHY
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