4U7T
 
 | | Crystal structure of DNMT3A-DNMT3L in complex with histone H3 | | Descriptor: | DNA (cytosine-5)-methyltransferase 3-like, DNA (cytosine-5)-methyltransferase 3A, S-ADENOSYL-L-HOMOCYSTEINE, ... | | Authors: | Guo, X, Wang, L, Yin, X, Li, J, Xiao, J, He, S, Wang, J, Xu, Y. | | Deposit date: | 2014-07-31 | | Release date: | 2014-11-12 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Structural insight into autoinhibition and histone H3-induced activation of DNMT3A
Nature, 517, 2015
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4XV2
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4UP0
 | | Ternary crystal structure of the Pygo2 PHD finger in complex with the B9L HD1 domain and a H3K4me2 peptide | | Descriptor: | HISTONE H3.1, PYGOPUS HOMOLOG 2, B-CELL CLL/LYMPHOMA 9-LIKE PROTEIN, ... | | Authors: | Miller, T.C.R, Fiedler, M, Rutherford, T.J, Birchall, K, Chugh, J, Bienz, M. | | Deposit date: | 2014-06-11 | | Release date: | 2014-11-05 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (1.28 Å) | | Cite: | Competitive Binding of a Benzimidazole to the Histone-Binding Pocket of the Pygo Phd Finger.
Acs Chem.Biol., 9, 2014
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3IDP
 | | B-Raf V600E kinase domain in complex with an aminoisoquinoline inhibitor | | Descriptor: | B-Raf proto-oncogene serine/threonine-protein kinase, N~1~-(4-chlorophenyl)-6-methyl-N~5~-[3-(7H-purin-6-yl)pyridin-2-yl]isoquinoline-1,5-diamine | | Authors: | Whittington, D.A, Epstein, L.F. | | Deposit date: | 2009-07-21 | | Release date: | 2009-10-06 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Selective inhibitors of the mutant B-raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline.
J.Med.Chem., 52, 2009
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3KQI
 | | crystal structure of PHF2 PHD domain complexed with H3K4Me3 peptide | | Descriptor: | CHLORIDE ION, GLYCEROL, H3K4Me3 peptide, ... | | Authors: | Wen, H, Li, J.Z, Song, T, Lu, M, Lee, M. | | Deposit date: | 2009-11-17 | | Release date: | 2010-02-02 | | Last modified: | 2019-02-13 | | Method: | X-RAY DIFFRACTION (1.78 Å) | | Cite: | Recognition of histone H3K4 trimethylation by the plant homeodomain of PHF2 modulates histone demethylation.
J.Biol.Chem., 285, 2010
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3KV4
 | | Structure of PHF8 in complex with histone H3 | | Descriptor: | 1,2-ETHANEDIOL, FE (II) ION, Histone H3-like, ... | | Authors: | Horton, J.R, Upadhyay, A.K, Qi, H.H, Zhang, X, Shi, Y, Cheng, X. | | Deposit date: | 2009-11-29 | | Release date: | 2009-12-22 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.19 Å) | | Cite: | Enzymatic and structural insights for substrate specificity of a family of jumonji histone lysine demethylases.
Nat.Struct.Mol.Biol., 17, 2010
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3LQJ
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3LQI
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6ZHX
 | | Cryo-EM structure of the regulatory linker of ALC1 bound to the nucleosome's acidic patch: nucleosome class. | | Descriptor: | Chromodomain-helicase-DNA-binding protein 1-like, DNA (145-MER) Widom 601 sequence, Histone H2A type 1, ... | | Authors: | Bacic, L, Gaullier, G, Croll, T.I, Deindl, S. | | Deposit date: | 2020-06-24 | | Release date: | 2020-12-23 | | Last modified: | 2021-07-14 | | Method: | ELECTRON MICROSCOPY (2.5 Å) | | Cite: | Mechanistic Insights into Regulation of the ALC1 Remodeler by the Nucleosome Acidic Patch.
Cell Rep, 33, 2020
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6ZHY
 | | Cryo-EM structure of the regulatory linker of ALC1 bound to the nucleosome's acidic patch: hexasome class. | | Descriptor: | Chromodomain-helicase-DNA-binding protein 1-like, DNA (110-MER) Widom 601 sequence, Histone H2A type 1, ... | | Authors: | Bacic, L, Gaullier, G, Deindl, S. | | Deposit date: | 2020-06-24 | | Release date: | 2020-12-23 | | Last modified: | 2021-07-14 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Mechanistic Insights into Regulation of the ALC1 Remodeler by the Nucleosome Acidic Patch.
Cell Rep, 33, 2020
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7A08
 | | CryoEM Structure of cGAS Nucleosome complex | | Descriptor: | Cyclic GMP-AMP synthase, Histone H2A type 1-C, Histone H2B type 1-C/E/F/G/I, ... | | Authors: | Michalski, S, de Oliveira Mann, C.C, Witte, G, Bartho, J, Lammens, K, Hopfner, K.P. | | Deposit date: | 2020-08-07 | | Release date: | 2020-09-23 | | Last modified: | 2021-02-10 | | Method: | ELECTRON MICROSCOPY (3.11 Å) | | Cite: | Structural basis for sequestration and autoinhibition of cGAS by chromatin.
Nature, 587, 2020
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7BU9
 | | Crystal Structure of Spindlin1-H3(K4me3-K9me2) complex | | Descriptor: | H3(K4me3-K9me2) peptide, Spindlin-1 | | Authors: | Zhao, F, Li, H. | | Deposit date: | 2020-04-05 | | Release date: | 2020-10-14 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (3.502 Å) | | Cite: | Molecular basis for histone H3 "K4me3-K9me3/2" methylation pattern readout by Spindlin1.
J.Biol.Chem., 295, 2020
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7BQZ
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7BG9
 | | The catalytic core lobe of human telomerase in complex with a telomeric DNA substrate | | Descriptor: | DNA (5'-D(P*TP*TP*AP*GP*GP*G)-3'), Histone H2A, Histone H2B, ... | | Authors: | Nguyen, T.H.D, Ghanim, G.E, Fountain, A.J, van Roon, A.M.M, Rangan, R, Das, R, Collins, K. | | Deposit date: | 2021-01-06 | | Release date: | 2021-04-28 | | Last modified: | 2024-05-01 | | Method: | ELECTRON MICROSCOPY (3.8 Å) | | Cite: | Structure of human telomerase holoenzyme with bound telomeric DNA.
Nature, 593, 2021
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6VO5
 | | Crystal structure of Human histone acetytransferas 1 (HAT1) in complex with isobutryl-COA and K12A mutant variant of histone H4 | | Descriptor: | ACETATE ION, GLYCEROL, Histone H4, ... | | Authors: | Halabelian, L, Zeng, H, Dong, A, Loppnau, P, Bountra, C, Edwards, A.M, Arrowsmith, C.H, Structural Genomics Consortium (SGC) | | Deposit date: | 2020-01-30 | | Release date: | 2020-03-11 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | Crystal structure of Human histone acetytransferas 1 (HAT1) in complex with isobutryl-COA and K12A mutant variant of histone H4
to be published
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3C4C
 | | B-Raf Kinase in Complex with PLX4720 | | Descriptor: | B-Raf proto-oncogene serine/threonine-protein kinase, N-{3-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl}propane-1-sulfonamide | | Authors: | Zhang, K.Y.J, Wang, W. | | Deposit date: | 2008-01-29 | | Release date: | 2008-02-26 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.57 Å) | | Cite: | Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity
Proc.Natl.Acad.Sci.Usa, 105, 2008
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6VYP
 | | Crystal structure of the LSD1/CoREST histone demethylase bound to its nucleosome substrate | | Descriptor: | DNA (191-MER), FLAVIN-ADENINE DINUCLEOTIDE, Histone H2A type 1, ... | | Authors: | Kim, S, Zhu, J, Eek, P, Yennawar, N, Song, T. | | Deposit date: | 2020-02-27 | | Release date: | 2020-05-27 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (4.99 Å) | | Cite: | Crystal Structure of the LSD1/CoREST Histone Demethylase Bound to Its Nucleosome Substrate.
Mol.Cell, 78, 2020
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3C1B
 | | The effect of H3 K79 dimethylation and H4 K20 trimethylation on nucleosome and chromatin structure | | Descriptor: | Histone 2, H2bf, Histone H2A type 1, ... | | Authors: | Lu, X, Simon, M, Chodaparambil, J, Hansen, J, Shokat, K, Luger, K. | | Deposit date: | 2008-01-22 | | Release date: | 2008-10-07 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | The effect of H3K79 dimethylation and H4K20 trimethylation on nucleosome and chromatin structure.
Nat.Struct.Mol.Biol., 15, 2008
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3C1C
 | | The effect of H3 K79 dimethylation and H4 K20 trimethylation on nucleosome and chromatin structure | | Descriptor: | Histone 2, H2bf, Histone H2A type 1, ... | | Authors: | Lu, X, Simon, M, Chodaparambil, J, Hansen, J, Shokat, K, Luger, K. | | Deposit date: | 2008-01-22 | | Release date: | 2008-10-07 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (3.15 Å) | | Cite: | The effect of H3K79 dimethylation and H4K20 trimethylation on nucleosome and chromatin structure.
Nat.Struct.Mol.Biol., 15, 2008
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3C9K
 | | Model of Histone Octamer Tubular Crystals | | Descriptor: | Histone H2A-IV, Histone H2B 7, Histone H3.2, ... | | Authors: | Frouws, T.D. | | Deposit date: | 2008-02-16 | | Release date: | 2009-01-06 | | Last modified: | 2024-03-13 | | Method: | ELECTRON MICROSCOPY (20 Å) | | Cite: | Histone octamer helical tubes suggest that an internucleosomal four-helix bundle stabilizes the chromatin fiber
Biophys.J., 96, 2009
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3D4Q
 | | Pyrazole-based inhibitors of B-Raf kinase | | Descriptor: | (1E)-5-(1-piperidin-4-yl-3-pyridin-4-yl-1H-pyrazol-4-yl)-2,3-dihydro-1H-inden-1-one oxime, B-Raf proto-oncogene serine/threonine-protein kinase | | Authors: | Morales, T, Vigers, G.P.A, Brandhuber, B.J. | | Deposit date: | 2008-05-14 | | Release date: | 2008-08-19 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Potent and selective pyrazole-based inhibitors of B-Raf kinase.
Bioorg.Med.Chem.Lett., 18, 2008
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6XAG
 | | Apo BRAF dimer bound to 14-3-3 | | Descriptor: | 1,2-ETHANEDIOL, 14-3-3 protein zeta/delta, Serine/threonine-protein kinase B-raf | | Authors: | Liau, N.P.D, Hymowitz, S.G, Sudhamsu, J. | | Deposit date: | 2020-06-04 | | Release date: | 2020-10-07 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (3.3 Å) | | Cite: | Dimerization Induced by C-Terminal 14-3-3 Binding Is Sufficient for BRAF Kinase Activation.
Biochemistry, 59, 2020
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3DB3
 | | Crystal structure of the tandem tudor domains of the E3 ubiquitin-protein ligase UHRF1 in complex with trimethylated histone H3-K9 peptide | | Descriptor: | E3 ubiquitin-protein ligase UHRF1, Trimethylated histone H3-K9 peptide | | Authors: | Walker, J.R, Avvakumov, G.V, Xue, S, Dong, A, Li, Y, Bountra, C, Weigelt, J, Arrowsmith, C.H, Edwards, A.M, Bochkarev, A, Dhe-Paganon, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2008-05-30 | | Release date: | 2008-09-16 | | Last modified: | 2012-04-18 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Recognition of multivalent histone states associated with heterochromatin by UHRF1 protein.
J.Biol.Chem., 286, 2011
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6XFP
 | | Crystal Structure of BRAF kinase domain bound to Belvarafenib | | Descriptor: | 4-amino-N-{1-[(3-chloro-2-fluorophenyl)amino]-6-methylisoquinolin-5-yl}thieno[3,2-d]pyrimidine-7-carboxamide, CHLORIDE ION, Serine/threonine-protein kinase B-raf | | Authors: | Yin, J, Sudhamsu, J. | | Deposit date: | 2020-06-16 | | Release date: | 2021-03-10 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | ARAF mutations confer resistance to the RAF inhibitor belvarafenib in melanoma.
Nature, 594, 2021
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6XLO
 | | Crystal structure of bRaf in complex with inhibitor | | Descriptor: | 3-(2-cyanopropan-2-yl)-N-[2-fluoro-4-methyl-5-(7-methyl-8-oxo-7,8-dihydropyrido[2,3-d]pyridazin-3-yl)phenyl]benzamide, IODIDE ION, Serine/threonine-protein kinase B-raf | | Authors: | Yin, J, Eigenbrot, C, Wang, W. | | Deposit date: | 2020-06-28 | | Release date: | 2021-05-26 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.493 Å) | | Cite: | Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3 H )-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor.
J.Med.Chem., 64, 2021
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