6R7I
 
 | | Structural basis of Cullin-2 RING E3 ligase regulation by the COP9 signalosome | | Descriptor: | COP9 signalosome complex subunit 1, COP9 signalosome complex subunit 2, COP9 signalosome complex subunit 3, ... | | Authors: | Faull, S.F, Lau, A.M.C, Beuron, F, Cronin, N.B, Morris, E.P, Politis, A. | | Deposit date: | 2019-03-28 | | Release date: | 2019-08-28 | | Last modified: | 2019-09-04 | | Method: | ELECTRON MICROSCOPY (5.9 Å) | | Cite: | Structural basis of Cullin 2 RING E3 ligase regulation by the COP9 signalosome.
Nat Commun, 10, 2019
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8IHT
 | | Rpd3S bound to the nucleosome | | Descriptor: | CALCIUM ION, Chromatin modification-related protein EAF3, DNA (164-MER), ... | | Authors: | Zhang, Y, Gang, C. | | Deposit date: | 2023-02-23 | | Release date: | 2024-03-20 | | Method: | ELECTRON MICROSCOPY (3.72 Å) | | Cite: | Structural basis for nucleosome binding and catalysis by the yeast Rpd3S/HDAC holoenzyme.
Cell Res., 33, 2023
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7O07
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8JHO
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7O7K
 | | Crystal structure of the human DYRK1A kinase domain bound to abemaciclib | | Descriptor: | 1,2-ETHANEDIOL, CITRATE ANION, DI(HYDROXYETHYL)ETHER, ... | | Authors: | Kaltheuner, I.H, Anand, K, Geyer, M. | | Deposit date: | 2021-04-13 | | Release date: | 2021-11-24 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.82 Å) | | Cite: | Abemaciclib is a potent inhibitor of DYRK1A and HIP kinases involved in transcriptional regulation.
Nat Commun, 12, 2021
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7O7I
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5L3B
 | | Human LSD1/CoREST: LSD1 D556G mutation | | Descriptor: | FLAVIN-ADENINE DINUCLEOTIDE, Lysine-specific histone demethylase 1A, REST corepressor 1 | | Authors: | Pilotto, S, Speranzini, V, Marabelli, C. | | Deposit date: | 2016-04-06 | | Release date: | 2016-05-04 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (3.3 Å) | | Cite: | LSD1/KDM1A mutations associated to a newly described form of intellectual disability impair demethylase activity and binding to transcription factors.
Hum.Mol.Genet., 25, 2016
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5L3D
 | | Human LSD1/CoREST: LSD1 Y761H mutation | | Descriptor: | FLAVIN-ADENINE DINUCLEOTIDE, Lysine-specific histone demethylase 1A, REST corepressor 1 | | Authors: | Pilotto, S, Speranzini, V, Marabelli, C, Mattevi, A. | | Deposit date: | 2016-04-06 | | Release date: | 2016-05-04 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | LSD1/KDM1A mutations associated to a newly described form of intellectual disability impair demethylase activity and binding to transcription factors.
Hum.Mol.Genet., 25, 2016
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7OWG
 | | human DEPTOR in a complex with mutant human mTORC1 A1459P | | Descriptor: | DEP domain-containing mTOR-interacting protein, Regulatory-associated protein of mTOR, Serine/threonine-protein kinase mTOR, ... | | Authors: | Heimhalt, M, Berndt, A, Wagstaff, J, Anandapadamanaban, M, Perisic, O, Maslen, S, McLaughlin, S, Yu, W.-H, Masson, G.R, Boland, A, Ni, X, Yamashita, K, Murshudov, G.N, Skehel, M, Freund, S.M, Williams, R.L. | | Deposit date: | 2021-06-18 | | Release date: | 2021-09-08 | | Last modified: | 2024-07-17 | | Method: | ELECTRON MICROSCOPY (4.7 Å) | | Cite: | Bipartite binding and partial inhibition links DEPTOR and mTOR in a mutually antagonistic embrace.
Elife, 10, 2021
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5L3C
 | | Human LSD1/CoREST: LSD1 E379K mutation | | Descriptor: | FLAVIN-ADENINE DINUCLEOTIDE, Lysine-specific histone demethylase 1A, REST corepressor 1 | | Authors: | Pilotto, S, Speranzini, V, Marabelli, C, Mattevi, A. | | Deposit date: | 2016-04-06 | | Release date: | 2016-05-04 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (3.31 Å) | | Cite: | LSD1/KDM1A mutations associated to a newly described form of intellectual disability impair demethylase activity and binding to transcription factors.
Hum.Mol.Genet., 25, 2016
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5LHG
 | | Structure of the KDM1A/CoREST complex with the inhibitor 4-methyl-N-[4-[[4-(1-methylpiperidin-4-yl)oxyphenoxy]methyl]phenyl]thieno[3,2-b]pyrrole-5-carboxamide | | Descriptor: | 4-methyl-N-[4-[[4-[(1-methyl-4-piperidyl)oxy]phenoxy]methyl]phenyl]thieno[3,2-b]pyrrole-5-carboxamide, FLAVIN-ADENINE DINUCLEOTIDE, GLYCEROL, ... | | Authors: | Cecatiello, V, Pasqualato, S. | | Deposit date: | 2016-07-11 | | Release date: | 2017-02-22 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (3.34 Å) | | Cite: | Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 2: Structure-Based Drug Design and Structure-Activity Relationship.
J. Med. Chem., 60, 2017
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5B33
 | | The crystal structure of the H2AZ nucleosome with H3.3. | | Descriptor: | DNA (146-MER), Histone H2A.Z, Histone H2B type 1-J, ... | | Authors: | Horikoshi, N, Taguchi, H, Arimura, Y, Kurumizaka, H. | | Deposit date: | 2016-02-08 | | Release date: | 2016-08-03 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2.925 Å) | | Cite: | Crystal structures of heterotypic nucleosomes containing histones H2A.Z and H2A.
Open Biology, 6, 2016
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5LHI
 | | Structure of the KDM1A/CoREST complex with the inhibitor N-[3-(ethoxymethyl)-2-[[4-[[(3R)-pyrrolidin-3-yl]methoxy]phenoxy]methyl]phenyl]-4-methylthieno[3,2-b]pyrrole-5-carboxamide | | Descriptor: | FLAVIN-ADENINE DINUCLEOTIDE, GLYCEROL, LYSINE-SPECIFIC HISTONE DEMETHYLASE 1, ... | | Authors: | Cecatiello, V, Pasqualato, S. | | Deposit date: | 2016-07-12 | | Release date: | 2017-02-22 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (3.4 Å) | | Cite: | Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 2: Structure-Based Drug Design and Structure-Activity Relationship.
J. Med. Chem., 60, 2017
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5LHH
 | | Structure of the KDM1A/CoREST complex with the inhibitor 4-ethyl-N-[3-(methoxymethyl)-2-[[4-[[(3R)-pyrrolidin-3-yl]methoxy]phenoxy]methyl]phenyl]thieno[3,2-b]pyrrole-5-carboxamide | | Descriptor: | 4-ethyl-~{N}-[3-(methoxymethyl)-2-[[4-[[(3~{R})-pyrrolidin-3-yl]methoxy]phenoxy]methyl]phenyl]thieno[3,2-b]pyrrole-5-carboxamide, FLAVIN-ADENINE DINUCLEOTIDE, GLYCEROL, ... | | Authors: | Cecatiello, V, Pasqualato, S. | | Deposit date: | 2016-07-11 | | Release date: | 2017-02-22 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (3.05 Å) | | Cite: | Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 2: Structure-Based Drug Design and Structure-Activity Relationship.
J. Med. Chem., 60, 2017
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8OKX
 | | Structure of cGAS in complex with SPSB3-ELOBC | | Descriptor: | Cyclic GMP-AMP synthase, Elongin-B, Elongin-C, ... | | Authors: | Xu, P.B, Ablasser, A. | | Deposit date: | 2023-03-29 | | Release date: | 2024-02-14 | | Last modified: | 2024-04-10 | | Method: | ELECTRON MICROSCOPY (3.51 Å) | | Cite: | The CRL5-SPSB3 ubiquitin ligase targets nuclear cGAS for degradation.
Nature, 627, 2024
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8OL1
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7PE9
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7PEB
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7PEC
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7PE8
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7PEA
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7PE7
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5MPA
 | | 26S proteasome in presence of ATP (s2) | | Descriptor: | 26S protease regulatory subunit 4 homolog, 26S protease regulatory subunit 6A, 26S protease regulatory subunit 6B homolog, ... | | Authors: | Wehmer, M, Rudack, T, Beck, F, Aufderheide, A, Pfeifer, G, Plitzko, J.M, Foerster, F, Schulten, K, Baumeister, W, Sakata, E. | | Deposit date: | 2016-12-16 | | Release date: | 2017-03-08 | | Last modified: | 2024-05-15 | | Method: | ELECTRON MICROSCOPY (4.5 Å) | | Cite: | Structural insights into the functional cycle of the ATPase module of the 26S proteasome.
Proc. Natl. Acad. Sci. U.S.A., 114, 2017
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5ML5
 | | Human p38alpha MAPK in complex with imidazolyl pyridine inhibitor 11b | | Descriptor: | 3-(2,5-dimethoxyphenyl)-~{N}-[4-[4-(4-fluorophenyl)-2-methylsulfanyl-1~{H}-imidazol-5-yl]pyridin-2-yl]propanamide, Mitogen-activated protein kinase 14, octyl beta-D-glucopyranoside | | Authors: | Buehrmann, M, Rauh, D. | | Deposit date: | 2016-12-06 | | Release date: | 2017-04-05 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Optimized 4,5-Diarylimidazoles as Potent/Selective Inhibitors of Protein Kinase CK1 delta and Their Structural Relation to p38 alpha MAPK.
Molecules, 22, 2017
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5MP9
 | | 26S proteasome in presence of ATP (s1) | | Descriptor: | 26S protease regulatory subunit 4 homolog, 26S protease regulatory subunit 6A, 26S protease regulatory subunit 6B homolog, ... | | Authors: | Wehmer, M, Rudack, T, Beck, F, Aufderheide, A, Pfeifer, G, Plitzko, J.M, Foerster, F, Schulten, K, Baumeister, W, Sakata, E. | | Deposit date: | 2016-12-16 | | Release date: | 2017-03-08 | | Last modified: | 2024-05-15 | | Method: | ELECTRON MICROSCOPY (4.1 Å) | | Cite: | Structural insights into the functional cycle of the ATPase module of the 26S proteasome.
Proc. Natl. Acad. Sci. U.S.A., 114, 2017
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