1Z83
 
 | | Crystal structure of human AK1A in complex with AP5A | | 分子名称: | Adenylate kinase 1, BIS(ADENOSINE)-5'-PENTAPHOSPHATE, SULFATE ION, ... | | 著者 | Filippakopoulos, P, Bunkoczi, G, Jansson, A, Schreurs, A, Knapp, S, Edwards, A, von Delft, F, Sundstrom, M, Structural Genomics Consortium (SGC) | | 登録日 | 2005-03-29 | | 公開日 | 2005-04-26 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Crystal structure of human AK1A in complex with AP5A
To be Published
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3BHH
 | | Crystal structure of human calcium/calmodulin-dependent protein kinase IIB isoform 1 (CAMK2B) | | 分子名称: | Calcium/calmodulin-dependent protein kinase type II beta chain, [4-({4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-6-(methylamino)pyrimidin-2-yl}amino)phenyl]acetonitrile | | 著者 | Filippakopoulos, P, Rellos, P, Niesen, F, Burgess, N, Bullock, A, Berridge, G, Pike, A.C.W, Ugochukwu, E, Pilka, E.S, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2007-11-28 | | 公開日 | 2007-12-11 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Crystal Structure of Human Calcium/Calmodulin-Dependent Protein Kinase IIB Isoform 1 (CAMK2B).
To be Published
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3BKB
 | | Crystal structure of human Feline Sarcoma Viral Oncogene Homologue (v-FES) | | 分子名称: | 1,2-ETHANEDIOL, Proto-oncogene tyrosine-protein kinase Fes/Fps, STAUROSPORINE, ... | | 著者 | Filippakopoulos, P, Salah, E, Fedorov, O, Cooper, C, Ugochukwu, E, Pike, A.C.W, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2007-12-06 | | 公開日 | 2007-12-25 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (1.78 Å) | | 主引用文献 | Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activation
Cell(Cambridge,Mass.), 134, 2008
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4MR3
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with a quinazolinone ligand (RVX-OH) | | 分子名称: | 1,2-ETHANEDIOL, 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxyquinazolin-4(3H)-one, Bromodomain-containing protein 4 | | 著者 | Filippakopoulos, P, Picaud, S, Felletar, I, Martin, S, Fedorov, O, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2013-09-17 | | 公開日 | 2013-11-27 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (1.68 Å) | | 主引用文献 | RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.
Proc.Natl.Acad.Sci.USA, 110, 2013
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4MR5
 | | Crystal Structure of the second bromodomain of human BRD2 in complex with a quinazolinone ligand (RVX-OH) | | 分子名称: | 1,2-ETHANEDIOL, 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxyquinazolin-4(3H)-one, Bromodomain-containing protein 2, ... | | 著者 | Filippakopoulos, P, Picaud, S, Felletar, I, Martin, S, Fedorov, O, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2013-09-17 | | 公開日 | 2013-11-27 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (1.63 Å) | | 主引用文献 | RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.
Proc.Natl.Acad.Sci.USA, 110, 2013
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4MR6
 | | Crystal Structure of the second bromodomain of human BRD2 in complex with a quinazolinone ligand (RVX-208) | | 分子名称: | 1,2-ETHANEDIOL, 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxyquinazolin-4(3H)-one, Bromodomain-containing protein 2, ... | | 著者 | Filippakopoulos, P, Picaud, S, Felletar, I, Martin, S, Fedorov, O, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2013-09-17 | | 公開日 | 2013-11-27 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (1.67 Å) | | 主引用文献 | RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.
Proc.Natl.Acad.Sci.USA, 110, 2013
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4MR4
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with a quinazolinone ligand (RVX-208) | | 分子名称: | 1,2-ETHANEDIOL, 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxyquinazolin-4(3H)-one, Bromodomain-containing protein 4 | | 著者 | Filippakopoulos, P, Picaud, S, Felletar, I, Martin, S, Fedorov, O, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2013-09-17 | | 公開日 | 2013-11-27 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (1.66 Å) | | 主引用文献 | RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.
Proc.Natl.Acad.Sci.USA, 110, 2013
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7AQB
 | | Crystal structure of human mitogen activated protein kinase 6 (MAPK6) | | 分子名称: | 1,2-ETHANEDIOL, MAGNESIUM ION, Mitogen-activated protein kinase 6 | | 著者 | Filippakopoulos, P, Schroeder, M, Chaikuad, A, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2020-10-20 | | 公開日 | 2020-11-11 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (2.25 Å) | | 主引用文献 | Crystal Structure and Inhibitor Identifications Reveal Targeting Opportunity for the Atypical MAPK Kinase ERK3.
Int J Mol Sci, 21, 2020
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5E7D
 | | Crystal Structure of the fifth bromodomain of human PB1 in complex with a hydroxyphenyl ligand | | 分子名称: | (2E)-3-(dimethylamino)-1-(2-hydroxyphenyl)prop-2-en-1-one, 1,2-ETHANEDIOL, Protein polybromo-1 | | 著者 | Filippakopoulos, P, Picaud, S, von Delft, F, Arrowsmith, C.H, Edwards, A, Bountra, C, Owen, D, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2015-10-12 | | 公開日 | 2016-10-12 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (1.87 Å) | | 主引用文献 | Crystal Structure of the fifth bromodomain of human PB1 in complex with a hydroxyphenyl ligand
To Be Published
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4Y03
 | | Crystal Structure of the fifth bromodomain of human PB1 in complex with salicylic acid | | 分子名称: | 2-HYDROXYBENZOIC ACID, CITRIC ACID, Protein polybromo-1 | | 著者 | Filippakopoulos, P, Picaud, S, Felletar, I, Fedorov, O, von Delft, F, Edwards, A.M, Arrowsmith, C.H, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2015-02-05 | | 公開日 | 2015-05-20 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (1.94 Å) | | 主引用文献 | Crystal Structure of the fifth bromodomain of human PB1 in complex with salicylic acid
To Be Published
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5NNC
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with a diacetylated histone 4 peptide (H3K9ac/K14ac) | | 分子名称: | Bromodomain-containing protein 4, Histone H3 | | 著者 | Filippakopoulos, P, Picaud, S, Pike, A.C.W, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C. | | 登録日 | 2017-04-08 | | 公開日 | 2018-05-16 | | 最終更新日 | 2024-10-16 | | 実験手法 | X-RAY DIFFRACTION (2.22 Å) | | 主引用文献 | Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains.
Mol. Cell, 73, 2019
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5NNG
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with an acetylated SRPK1 peptide (K585ac) | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, VAG(ALY)YS(ALY)EFFY | | 著者 | Filippakopoulos, P, Picaud, S, Newman, J, Sorrell, F, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Structural Genomics Consortium (SGC) | | 登録日 | 2017-04-08 | | 公開日 | 2018-05-16 | | 最終更新日 | 2024-10-23 | | 実験手法 | X-RAY DIFFRACTION (1.2 Å) | | 主引用文献 | Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains.
Mol. Cell, 73, 2019
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5NNF
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with an acetylated BAZ1B peptide (K221ac) | | 分子名称: | Bromodomain-containing protein 4, FLPH(ALY)YDVKL | | 著者 | Filippakopoulos, P, Picaud, S, Krojer, T, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C. | | 登録日 | 2017-04-08 | | 公開日 | 2018-05-16 | | 最終更新日 | 2024-10-16 | | 実験手法 | X-RAY DIFFRACTION (1.15 Å) | | 主引用文献 | Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains.
Mol. Cell, 73, 2019
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5NND
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with a diacetylated histone 4 peptide (H3K9ac/K14ac) | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, Histone H3 | | 著者 | Filippakopoulos, P, Picaud, S, Pike, A.C.W, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C. | | 登録日 | 2017-04-08 | | 公開日 | 2018-05-16 | | 最終更新日 | 2024-10-16 | | 実験手法 | X-RAY DIFFRACTION (1.82 Å) | | 主引用文献 | Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains.
Mol. Cell, 73, 2019
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5NNE
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with a diacetylated TOP2A peptide (K1201ac/K1204ac) | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, GKA(ALY)GK(ALY)TQMY | | 著者 | Filippakopoulos, P, Picaud, S, Krojer, T, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C. | | 登録日 | 2017-04-08 | | 公開日 | 2018-05-16 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.15 Å) | | 主引用文献 | Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains.
Mol. Cell, 73, 2019
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2JK9
 | | The structure of splA-ryanodine receptor domain and SOCS box containing 1 in complex with a PAR-4 peptide | | 分子名称: | PRKC APOPTOSIS WT1 REGULATOR PROTEIN, SPRY DOMAIN-CONTAINING SOCS BOX PROTEIN 1 | | 著者 | Filippakopoulos, P, Bullock, A, Keates, T, Savitsky, P, Murray, J.W, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Wickstroem, M, Bountra, C, Knapp, S. | | 登録日 | 2008-08-22 | | 公開日 | 2008-09-16 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (1.79 Å) | | 主引用文献 | Structural Basis for Par-4 Recognition by the Spry Domain-and Socs Box-Containing Proteins Spsb1, Spsb2, and Spsb4.
J.Mol.Biol., 401, 2010
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6FSY
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with a 3,5-dimethylisoxazol ligand | | 分子名称: | 1,2-ETHANEDIOL, 3-(3,5-dimethyl-1,2-oxazol-4-yl)-5-[(~{R})-oxidanyl(pyridin-3-yl)methyl]phenol, Bromodomain-containing protein 4 | | 著者 | Filippakopoulos, P, Picaud, S, Conway, S.J, Pike, A.C.W, Krojer, T, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Structural Genomics Consortium (SGC) | | 登録日 | 2018-02-20 | | 公開日 | 2018-04-18 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.34 Å) | | 主引用文献 | BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.
Bioorg.Med.Chem., 26, 2018
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6FT4
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with a 3,5-dimethylisoxazol ligand | | 分子名称: | 3-[[4,4-bis(fluoranyl)piperidin-1-yl]methyl]-5-(3,5-dimethyl-1,2-oxazol-4-yl)phenol, Bromodomain-containing protein 4 | | 著者 | Filippakopoulos, P, Picaud, S, Pike, A.C.W, Krojer, T, Conway, S.J, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C. | | 登録日 | 2018-02-20 | | 公開日 | 2018-04-18 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.34 Å) | | 主引用文献 | BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.
Bioorg.Med.Chem., 26, 2018
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6G0O
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with an acetylated ATRX peptide (K1030ac/K1033ac) | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, Transcriptional regulator ATRX | | 著者 | Filippakopoulos, P, Picaud, S, Newman, J, Sorrell, F, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C. | | 登録日 | 2018-03-19 | | 公開日 | 2018-11-28 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.4 Å) | | 主引用文献 | Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains.
Mol. Cell, 73, 2019
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6G0P
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with an acetylated E2F1 peptide (K117ac/K120ac) | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, Transcription factor E2F1 | | 著者 | Filippakopoulos, P, Picaud, S, Krojer, T, Sorrell, F, Pike, A.C.W, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C. | | 登録日 | 2018-03-19 | | 公開日 | 2018-11-28 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.3 Å) | | 主引用文献 | Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains.
Mol. Cell, 73, 2019
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6G0Q
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with an acetylated GATA1 peptide (K312ac/K315ac) | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, Erythroid transcription factor | | 著者 | Filippakopoulos, P, Picaud, S, Newman, J, Sorrell, F, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C. | | 登録日 | 2018-03-19 | | 公開日 | 2018-11-28 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.4 Å) | | 主引用文献 | Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains.
Mol. Cell, 73, 2019
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6G0R
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with an acetylated POLR2A peptide (K775ac/K778ac) | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, DNA-directed RNA polymerase II subunit RPB1 | | 著者 | Filippakopoulos, P, Picaud, S, Pike, A.C.W, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C. | | 登録日 | 2018-03-19 | | 公開日 | 2018-11-28 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.25 Å) | | 主引用文献 | Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains.
Mol. Cell, 73, 2019
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6FT3
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with a 3,5-dimethylisoxazol ligand | | 分子名称: | 1,2-ETHANEDIOL, 3-[(~{R})-cyclopropyl(oxidanyl)methyl]-5-(3,5-dimethyl-1,2-oxazol-4-yl)phenol, Bromodomain-containing protein 4 | | 著者 | Filippakopoulos, P, Picaud, S, Pike, A.C.W, Krojer, T, Conway, S.J, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Structural Genomics Consortium (SGC) | | 登録日 | 2018-02-20 | | 公開日 | 2018-04-18 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.28 Å) | | 主引用文献 | BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.
Bioorg.Med.Chem., 26, 2018
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6G0S
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with an acetylated SIRT7 peptide (K272ac/K275ac) | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, NAD-dependent protein deacetylase sirtuin-7 | | 著者 | Filippakopoulos, P, Picaud, S, Krojer, T, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C. | | 登録日 | 2018-03-19 | | 公開日 | 2018-11-28 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.48 Å) | | 主引用文献 | Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains.
Mol. Cell, 73, 2019
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5TB6
 | | Structure of bromodomain of CREBBP with a pyrazolo[4,3-c]pyridin fragment | | 分子名称: | 1,2-ETHANEDIOL, 1-(3-phenyl-1,4,6,7-tetrahydropyrazolo[4,3-c]pyridin-5-yl)propan-1-one, CREB-binding protein | | 著者 | Filippakopoulos, P, Picaud, S, Knapp, S, von Delft, F, Bountra, C, Arrowsmith, C.H, Edwards, A, Structural Genomics Consortium (SGC) | | 登録日 | 2016-09-11 | | 公開日 | 2016-10-12 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.79 Å) | | 主引用文献 | Discovery of New Bromodomain Scaffolds by Biosensor Fragment Screening.
ACS Med Chem Lett, 7, 2016
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