7L5E
 
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7KK4
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8OKF
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7KHL
 | | BRD4-BD1 Compound6 (methyl 4-(3,5-difluoropyridin-2-yl)-10-methyl-7-((methylsulfonyl)methyl)-11-oxo-3,4,10,11-tetrahydro-1H-1,4,10-triazadibenzo[cd,f]azulene-6-carboxylate) | | 分子名称: | Bromodomain-containing protein 4, GLYCEROL, methyl 7-(3,5-difluoropyridin-2-yl)-2-methyl-10-[(methylsulfonyl)methyl]-3-oxo-3,4,6,7-tetrahydro-2H-2,4,7-triazadibenzo[cd,f]azulene-9-carboxylate | | 著者 | Murray, J.M. | | 登録日 | 2020-10-21 | | 公開日 | 2021-02-24 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (1.286 Å) | | 主引用文献 | Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy.
J.Med.Chem., 64, 2021
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7KHH
 | | Ternary complex of VHL/BRD4-BD1/Compound9 (4-(3,5-difluoropyridin-2-yl)-N-(11-(((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-11-oxoundecyl)-10-methyl-7-((methylsulfonyl)methyl)-11-oxo-3,4,10,11-tetrahydro-1H-1,4,10-triazadibenzo[cd,f]azulene-6-carboxamide) | | 分子名称: | Bromodomain-containing protein 4, Elongin-B, Elongin-C, ... | | 著者 | Murray, J.M. | | 登録日 | 2020-10-21 | | 公開日 | 2021-02-24 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.281 Å) | | 主引用文献 | Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy.
J.Med.Chem., 64, 2021
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7KZR
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8OK1
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8OK2
 | | Bipartite interaction of TOPBP1 with the GINS complex | | 分子名称: | DNA replication complex GINS protein PSF1, DNA replication complex GINS protein PSF2, DNA replication complex GINS protein PSF3, ... | | 著者 | Day, M, Oliver, A.W, Pearl, L.H. | | 登録日 | 2023-03-26 | | 公開日 | 2024-03-13 | | 実験手法 | ELECTRON MICROSCOPY (4.1 Å) | | 主引用文献 | TopBP1 utilises a bipartite GINS binding mode to support genome replication.
Nat Commun, 15, 2024
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7L1A
 | | Human Methionine Adenosyltransferase 2A bound to Methylthioadenosine and inhibitor, di-imido triphosphate (PNPNP) | | 分子名称: | 5'-DEOXY-5'-METHYLTHIOADENOSINE, ALANINE, MAGNESIUM ION, ... | | 著者 | Niland, C.N, Fedorov, E, Schramm, V.L, Ghosh, A. | | 登録日 | 2020-12-14 | | 公開日 | 2021-03-17 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (1.25 Å) | | 主引用文献 | Mechanism and Inhibition of Human Methionine Adenosyltransferase 2A.
Biochemistry, 60, 2021
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8Q1N
 | | Cyclic peptide binder of the WBM-site of WDR5 | | 分子名称: | Cyclic peptide inhibitor, WD repeat-containing protein 5 | | 著者 | Schmeing, S, Chang, J.Y, t Hart, P, Gasper, R. | | 登録日 | 2023-08-01 | | 公開日 | 2023-09-06 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (1.843 Å) | | 主引用文献 | Macrocyclic peptides as inhibitors of WDR5-lncRNA interactions.
Chem.Commun.(Camb.), 59, 2023
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7L5W
 | | p97-R155H mutant dodecamer I | | 分子名称: | Transitional endoplasmic reticulum ATPase | | 著者 | Nandi, P, Li, S, Coulmbres, R.C.A, Wang, F, Williams, D.R, Malyutin, A.G, Poh, Y.-P, Chou, T.-F, Chiu, P.-L. | | 登録日 | 2020-12-23 | | 公開日 | 2021-08-04 | | 最終更新日 | 2024-05-29 | | 実験手法 | ELECTRON MICROSCOPY (3.34 Å) | | 主引用文献 | Structural and Functional Analysis of Disease-Linked p97 ATPase Mutant Complexes.
Int J Mol Sci, 22, 2021
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7L5X
 | | p97-R155H mutant dodecamer II | | 分子名称: | Transitional endoplasmic reticulum ATPase | | 著者 | Nandi, P, Li, S, Coulmbres, R.C.A, Wang, F, Williams, D.R, Malyutin, A.G, Poh, Y.-P, Chou, T.-F, Chiu, P.-L. | | 登録日 | 2020-12-23 | | 公開日 | 2021-08-04 | | 最終更新日 | 2024-05-29 | | 実験手法 | ELECTRON MICROSCOPY (6.1 Å) | | 主引用文献 | Structural and Functional Analysis of Disease-Linked p97 ATPase Mutant Complexes.
Int J Mol Sci, 22, 2021
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7L7I
 | | Cryo-EM structure of Hsp90:FKBP51:p23 closed-state complex | | 分子名称: | Heat shock protein HSP 90-alpha, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, Peptidyl-prolyl cis-trans isomerase FKBP5, ... | | 著者 | Lee, K, Thwin, A.C, Tse, E, Gates, S.N, Southworth, D.R. | | 登録日 | 2020-12-28 | | 公開日 | 2021-08-25 | | 最終更新日 | 2024-05-29 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | The structure of an Hsp90-immunophilin complex reveals cochaperone recognition of the client maturation state.
Mol.Cell, 81, 2021
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8PXM
 | | N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH (1R,1'R)-7,7'-(pentane-1,5-diylbis(oxy))bis(1,3-dimethyl-1,3-dihydro-2H-benzo[d]azepin-2-one) | | 分子名称: | (1R)-7-[5-[[(1R)-1,3-dimethyl-2-oxidanylidene-1H-3-benzazepin-7-yl]oxy]pentoxy]-1,3-dimethyl-1H-3-benzazepin-2-one, 1,2-ETHANEDIOL, Bromodomain-containing protein 4 | | 著者 | Chung, C.W. | | 登録日 | 2023-07-23 | | 公開日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.378 Å) | | 主引用文献 | Design and Characterization of 1,3-Dihydro-2 H -benzo[ d ]azepin-2-ones as Rule-of-5 Compliant Bivalent BET Inhibitors.
Acs Med.Chem.Lett., 14, 2023
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8PXA
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7KTR
 | | Cryo-EM structure of the human SAGA coactivator complex (TRRAP, core) | | 分子名称: | Ataxin-7, INOSITOL HEXAKISPHOSPHATE, Isoform 3 of Transcription factor SPT20 homolog, ... | | 著者 | Herbst, D.A, Esbin, M.N, Nogales, E. | | 登録日 | 2020-11-24 | | 公開日 | 2021-11-10 | | 最終更新日 | 2024-05-29 | | 実験手法 | ELECTRON MICROSCOPY (2.93 Å) | | 主引用文献 | Structure of the human SAGA coactivator complex.
Nat.Struct.Mol.Biol., 28, 2021
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8PQN
 | | NQO1 bound to RBS-10 | | 分子名称: | FLAVIN-ADENINE DINUCLEOTIDE, NAD(P)H dehydrogenase [quinone] 1, ~{N}-[4-[(3-methylphenyl)carbonylamino]phenyl]-5-nitro-furan-2-carboxamide | | 著者 | Pous, J, Jose-Duran, F, Mayor-Ruiz, C, Riera, A. | | 登録日 | 2023-07-11 | | 公開日 | 2024-01-10 | | 最終更新日 | 2024-03-20 | | 実験手法 | X-RAY DIFFRACTION (3.8 Å) | | 主引用文献 | Discovery and Mechanistic Elucidation of NQO1-Bioactivatable Small Molecules That Overcome Resistance to Degraders.
Angew.Chem.Int.Ed.Engl., 63, 2024
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8PMP
 | | Structure of the human nuclear cap-binding complex bound to ARS2[147-871] and m7GTP | | 分子名称: | 7N-METHYL-8-HYDROGUANOSINE-5'-TRIPHOSPHATE, Nuclear cap-binding protein subunit 1, Nuclear cap-binding protein subunit 2, ... | | 著者 | Dubiez, E, Pellegrini, E, Foucher, A.E, Cusack, S, Kadlec, J. | | 登録日 | 2023-06-29 | | 公開日 | 2024-01-17 | | 実験手法 | ELECTRON MICROSCOPY (3.43 Å) | | 主引用文献 | Structural basis for competitive binding of productive and degradative co-transcriptional effectors to the nuclear cap-binding complex.
Cell Rep, 43, 2024
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7L72
 | | Crystal structure of the second bromodomain (BD2) of human BRD3 bound to Ro3280 | | 分子名称: | 4-[(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide, Bromodomain-containing protein 3 | | 著者 | Karim, M.R, Bikowitz, M, Schonbrunn, E. | | 登録日 | 2020-12-25 | | 公開日 | 2021-11-17 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (1.5 Å) | | 主引用文献 | Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
J.Med.Chem., 64, 2021
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8Q34
 | | Crystal structure of the first bromodomain of human BRD4 in complex with the ligand ZZ001229a | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, ~{N}-(1~{H}-imidazo[4,5-b]pyridin-2-ylmethyl)-3-(3-methyl-1,2-diazirin-3-yl)propanamide | | 著者 | MacLean, E.M, Gao, Q, Williams, E, Balcomb, B.H, von Delft, F, Bajusz, D, Keeley, A, Abranyi-Balogh, P, Koekemoer, L, Keseru, G.M. | | 登録日 | 2023-08-03 | | 公開日 | 2024-02-07 | | 最終更新日 | 2024-08-14 | | 実験手法 | X-RAY DIFFRACTION (1.48 Å) | | 主引用文献 | Mapping protein binding sites by photoreactive fragment pharmacophores.
Commun Chem, 7, 2024
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8PR4
 | | Dynactin pointed end bound to JIP3 | | 分子名称: | ADENOSINE-5'-TRIPHOSPHATE, Arp11, C-Jun-amino-terminal kinase-interacting protein 3, ... | | 著者 | Singh, K, Lau, C.K, Manigrasso, G, Gassmann, R, Carter, A.P. | | 登録日 | 2023-07-12 | | 公開日 | 2024-03-27 | | 最終更新日 | 2024-04-10 | | 実験手法 | ELECTRON MICROSCOPY (3.5 Å) | | 主引用文献 | Molecular mechanism of dynein-dynactin complex assembly by LIS1.
Science, 383, 2024
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8PXX
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8PXW
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8PN9
 | | Structure of human oligosaccharyltransferase OST-A complex bound to NGI-1 | | 分子名称: | (2E,6E,10E,14E,18E,22E,26E)-3,7,11,15,19,23,27,31-OCTAMETHYLDOTRIACONTA-2,6,10,14,18,22,26,30-OCTAENYL TRIHYDROGEN DIPHOSPHATE, (2~{S},3~{R},4~{R},5~{S},6~{S})-2-(hydroxymethyl)-6-[(1~{S},2~{R},3~{R},4~{R},5'~{S},6~{S},7~{R},8~{S},9~{R},12~{R},13~{R},15~{S},16~{S},18~{R})-5',7,9,13-tetramethyl-3,15-bis(oxidanyl)spiro[5-oxapentacyclo[10.8.0.0^{2,9}.0^{4,8}.0^{13,18}]icosane-6,2'-oxane]-16-yl]oxy-oxane-3,4,5-triol, (4R,7R)-4-hydroxy-N,N,N-trimethyl-4,9-dioxo-7-[(undecanoyloxy)methyl]-3,5,8-trioxa-4lambda~5~-phosphadocosan-1-aminium, ... | | 著者 | Ramirez, A.S, Kowal, J, Locher, K.P. | | 登録日 | 2023-06-30 | | 公開日 | 2024-05-08 | | 実験手法 | ELECTRON MICROSCOPY (3.61 Å) | | 主引用文献 | Positive selection CRISPR screens reveal a druggable pocket in an oligosaccharyltransferase required for inflammatory signaling to NF-kappa B.
Cell, 187, 2024
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7LMM
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