8EWV
 
 | | DNA-encoded library (DEL)-enabled discovery of proximity inducing small molecules | | Descriptor: | Bromodomain-containing protein 4, Elongin-B, Elongin-C, ... | | Authors: | Schreiber, S.L, Shu, W, Ma, X, Michaud, G, Bonazzi, S, Berst, F. | | Deposit date: | 2022-10-24 | | Release date: | 2023-10-04 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (3.4 Å) | | Cite: | DNA-encoded library-enabled discovery of proximity-inducing small molecules.
Nat.Chem.Biol., 20, 2024
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8R5H
 | | Ubiquitin ligation to neosubstrate by a cullin-RING E3 ligase & Cdc34: NEDD8-CUL2-RBX1-ELOB/C-VHL-MZ1 with trapped UBE2R2~donor UB-BRD4 BD2 | | Descriptor: | (2~{S},4~{R})-1-[(2~{S})-2-[2-[2-[2-[2-[2-[(9~{S})-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.0^{2,6}]trideca-2(6),4,7,10,12-pentaen-9-yl]ethanoylamino]ethoxy]ethoxy]ethoxy]ethanoylamino]-3,3-dimethyl-butanoyl]-~{N}-[[4-(4-methyl-2,3-dihydro-1,3-thiazol-5-yl)phenyl]methyl]-4-oxidanyl-pyrrolidine-2-carboxamide, 5-azanylpentan-2-one, Bromodomain-containing protein 4, ... | | Authors: | Liwocha, J, Prabu, J.R, Kleiger, G, Schulman, B.A. | | Deposit date: | 2023-11-16 | | Release date: | 2024-02-21 | | Last modified: | 2024-04-17 | | Method: | ELECTRON MICROSCOPY (3.44 Å) | | Cite: | Cullin-RING ligases employ geometrically optimized catalytic partners for substrate targeting.
Mol.Cell, 84, 2024
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6SIS
 | | Crystal structure of macrocyclic PROTAC 1 in complex with the second bromodomain of human Brd4 and pVHL:ElonginC:ElonginB | | Descriptor: | Bromodomain-containing protein 4, Elongin-B, Elongin-C, ... | | Authors: | Hughes, S.J, Testa, A, Ciulli, A. | | Deposit date: | 2019-08-10 | | Release date: | 2019-12-04 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (3.5 Å) | | Cite: | Structure-Based Design of a Macrocyclic PROTAC.
Angew.Chem.Int.Ed.Engl., 59, 2020
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6BN7
 | | Crystal structure of DDB1-CRBN-BRD4(BD1) complex bound to dBET23 PROTAC. | | Descriptor: | Bromodomain-containing protein 4, DNA damage-binding protein 1, Protein cereblon, ... | | Authors: | Nowak, R.P, DeAngelo, S.L, Buckley, D, Bradner, J.E, Fischer, E.S. | | Deposit date: | 2017-11-16 | | Release date: | 2018-05-30 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (3.501 Å) | | Cite: | Plasticity in binding confers selectivity in ligand-induced protein degradation.
Nat. Chem. Biol., 14, 2018
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8RX0
 | | (NEDD8)-CRL2VHL-MZ1-Brd4BD2-Ub(G76S, K48C)-UBE2R1(C93K, S138C, C191S, C223S)-Ub | | Descriptor: | (2~{S},4~{R})-1-[(2~{S})-2-[2-[2-[2-[2-[2-[(9~{S})-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.0^{2,6}]trideca-2(6),4,7,10,12-pentaen-9-yl]ethanoylamino]ethoxy]ethoxy]ethoxy]ethanoylamino]-3,3-dimethyl-butanoyl]-~{N}-[[4-(4-methyl-2,3-dihydro-1,3-thiazol-5-yl)phenyl]methyl]-4-oxidanyl-pyrrolidine-2-carboxamide, Cullin-2, Elongin-B, ... | | Authors: | Crowe, C, Nakasone, M.A. | | Deposit date: | 2024-02-05 | | Release date: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (3.7 Å) | | Cite: | (NEDD8)-CRL2VHL-MZ1-Brd4BD2-Ub(G76S, K48C)-UBE2R1(C93K, S138C, C191S, C223S)-Ub
To Be Published
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8OV6
 | | Ternary structure of intramolecular bivalent glue degrader IBG1 bound to BRD4 and DCAF16:DDB1deltaBPB | | Descriptor: | Bromodomain-containing protein 4, DDB1- and CUL4-associated factor 16, DDB1deltaBPB, ... | | Authors: | Cowan, A.D, Sundaramoorthy, R, Nakasone, M.A, Ciulli, A. | | Deposit date: | 2023-04-25 | | Release date: | 2023-05-17 | | Last modified: | 2024-03-13 | | Method: | ELECTRON MICROSCOPY (3.77 Å) | | Cite: | Targeted protein degradation via intramolecular bivalent glues.
Nature, 627, 2024
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6BN8
 | | Crystal structure of DDB1-CRBN-BRD4(BD1) complex bound to dBET55 PROTAC. | | Descriptor: | Bromodomain-containing protein 4, DNA damage-binding protein 1,DNA damage-binding protein 1, Protein cereblon, ... | | Authors: | Nowak, R.P, DeAngelo, S.L, Buckley, D, Bradner, J.E, Fischer, E.S. | | Deposit date: | 2017-11-16 | | Release date: | 2018-06-06 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (3.990035 Å) | | Cite: | Plasticity in binding confers selectivity in ligand-induced protein degradation.
Nat. Chem. Biol., 14, 2018
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8RWZ
 | | Open non-crosslinked structure Brd4BD2-MZ1-(NEDD8)-CRL2VHL | | Descriptor: | (2~{S},4~{R})-1-[(2~{S})-2-[2-[2-[2-[2-[2-[(9~{S})-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.0^{2,6}]trideca-2(6),4,7,10,12-pentaen-9-yl]ethanoylamino]ethoxy]ethoxy]ethoxy]ethanoylamino]-3,3-dimethyl-butanoyl]-~{N}-[[4-(4-methyl-2,3-dihydro-1,3-thiazol-5-yl)phenyl]methyl]-4-oxidanyl-pyrrolidine-2-carboxamide, Bromodomain-containing protein 4, Cullin-2, ... | | Authors: | Ciulli, A, Crowe, C, Nakacone, M.A. | | Deposit date: | 2024-02-05 | | Release date: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (4 Å) | | Cite: | Open non-crosslinked structure Brd4BD2-MZ1-(NEDD8)-CRL2VHL
To Be Published
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6BN9
 | | Crystal structure of DDB1-CRBN-BRD4(BD1) complex bound to dBET70 PROTAC | | Descriptor: | Bromodomain-containing protein 4, DNA damage-binding protein 1,DNA damage-binding protein 1, Protein cereblon, ... | | Authors: | Nowak, R.P, DeAngelo, S.L, Buckley, D, Bradner, J.E, Fischer, E.S. | | Deposit date: | 2017-11-16 | | Release date: | 2018-05-30 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (4.382 Å) | | Cite: | Plasticity in binding confers selectivity in ligand-induced protein degradation.
Nat. Chem. Biol., 14, 2018
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6BNB
 | | Crystal structure of DDB1-CRBN-BRD4(BD1) complex bound to dBET57 PROTAC | | Descriptor: | Bromodomain-containing protein 4, DNA damage-binding protein 1, Protein cereblon, ... | | Authors: | Nowak, R.P, DeAngelo, S.L, Buckley, D, Ishoey, M, He, Z, Zhang, T, Bradner, J.E, Fischer, E.S. | | Deposit date: | 2017-11-16 | | Release date: | 2018-05-30 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (6.343 Å) | | Cite: | Plasticity in binding confers selectivity in ligand-induced protein degradation.
Nat. Chem. Biol., 14, 2018
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6BNH
 | | Solution NMR structures of BRD4 ET domain with JMJD6 peptide | | Descriptor: | Bifunctional arginine demethylase and lysyl-hydroxylase JMJD6, Bromodomain-containing protein 4 | | Authors: | Konuma, T, Yu, D, Zhao, C, Ju, Y, Sharma, R, Ren, C, Zhang, Q, Zhou, M.-M, Zeng, L. | | Deposit date: | 2017-11-16 | | Release date: | 2017-12-20 | | Last modified: | 2024-05-15 | | Method: | SOLUTION NMR | | Cite: | Structural Mechanism of the Oxygenase JMJD6 Recognition by the Extraterminal (ET) Domain of BRD4.
Sci Rep, 7, 2017
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2LSP
 | | solution structures of BRD4 second bromodomain with NF-kB-K310ac peptide | | Descriptor: | Bromodomain-containing protein 4, NF-kB-K310ac peptide | | Authors: | Zhang, G, Liu, R, Zhong, Y, Plotnikov, A.N, Zhang, W, Rusinova, E, Gerona-Nevarro, G, Moshkina, N, Joshua, J, Chuang, P.Y, Ohlmeyer, M, He, J, Zhou, M.-M. | | Deposit date: | 2012-05-03 | | Release date: | 2012-07-18 | | Last modified: | 2023-11-15 | | Method: | SOLUTION NMR | | Cite: | Down-regulation of NF-kappa B transcriptional activity in HIV-associated kidney disease by BRD4 inhibition.
J.Biol.Chem., 287, 2012
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6MNL
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7AQT
 | | NMR2 structure of BRD4-BD2 in complex with iBET-762 | | Descriptor: | 2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide, Bromodomain-containing protein 4 | | Authors: | Orts, J, Torres, F, Milbradt, A.G, Walser, R. | | Deposit date: | 2020-10-23 | | Release date: | 2022-03-02 | | Last modified: | 2024-06-19 | | Method: | SOLUTION NMR | | Cite: | NMR Molecular Replacement Provides New Insights into Binding Modes to Bromodomains of BRD4 and TRIM24.
J.Med.Chem., 65, 2022
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2N3K
 | | Human Brd4 ET domain in complex with MLV Integrase C-term | | Descriptor: | Bromodomain-containing protein 4, MLV integrase | | Authors: | Crowe, B.L, Foster, M.P. | | Deposit date: | 2015-06-03 | | Release date: | 2016-03-02 | | Last modified: | 2024-05-15 | | Method: | SOLUTION NMR | | Cite: | Structure of the Brd4 ET domain bound to a C-terminal motif from gamma-retroviral integrases reveals a conserved mechanism of interaction.
Proc.Natl.Acad.Sci.USA, 113, 2016
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2ND0
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2NCZ
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2ND1
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5Z9C
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2MJV
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2I8N
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