7LMK
 
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8Q1H
 | | LSD1 Y391K-CoREST bound to Histone H3 N-terminal tail | | Descriptor: | FLAVIN-ADENINE DINUCLEOTIDE, Histone H3.3C, Lysine-specific histone demethylase 1A, ... | | Authors: | Barone, M, Mattevi, A. | | Deposit date: | 2023-07-31 | | Release date: | 2024-05-15 | | Last modified: | 2024-07-17 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Uncoupling histone modification crosstalk by engineering lysine demethylase LSD1.
Nat.Chem.Biol., 2024
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8Q1G
 | | LSD1-CoREST bound to Acetylated K14 of Histone H3 | | Descriptor: | FLAVIN-ADENINE DINUCLEOTIDE, Histone H3.3C, Lysine-specific histone demethylase 1A, ... | | Authors: | Barone, M, Mattevi, A. | | Deposit date: | 2023-07-31 | | Release date: | 2024-05-15 | | Last modified: | 2024-07-17 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Uncoupling histone modification crosstalk by engineering lysine demethylase LSD1.
Nat.Chem.Biol., 2024
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8PQX
 | | p97 (VCP) mutant - F539A state III | | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, ADENOSINE-5'-TRIPHOSPHATE, Transitional endoplasmic reticulum ATPase | | Authors: | Arie, M, Matzov, D, Karmona, R, Szenkier, N, Stanhill, A, Navon, A. | | Deposit date: | 2023-07-12 | | Release date: | 2024-05-29 | | Method: | ELECTRON MICROSCOPY (3.3 Å) | | Cite: | p97 (VCP) mutant - F539A state III
To Be Published
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8Q1J
 | | LSD1 Y391K-CoREST bound to Acetylated K14 of Histone H3 | | Descriptor: | FLAVIN-ADENINE DINUCLEOTIDE, Histone H3.3C, Lysine-specific histone demethylase 1A, ... | | Authors: | Barone, M, Mattevi, A. | | Deposit date: | 2023-07-31 | | Release date: | 2024-05-15 | | Last modified: | 2024-07-17 | | Method: | X-RAY DIFFRACTION (2.87 Å) | | Cite: | Uncoupling histone modification crosstalk by engineering lysine demethylase LSD1.
Nat.Chem.Biol., 2024
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7LU5
 | | SAMHD1(113-626) H206R D207N R366H | | Descriptor: | 2'-DEOXYGUANOSINE-5'-TRIPHOSPHATE, Deoxynucleoside triphosphate triphosphohydrolase SAMHD1 | | Authors: | Temple, J.T, Bowen, N.E. | | Deposit date: | 2021-02-20 | | Release date: | 2021-11-24 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (3.57 Å) | | Cite: | Structural and functional characterization explains loss of dNTPase activity of the cancer-specific R366C/H mutant SAMHD1 proteins.
J.Biol.Chem., 297, 2021
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8PK5
 | | INTS13-INTS14 complex with ZNF609 | | Descriptor: | Integrator complex subunit 13, Integrator complex subunit 14,Zinc finger protein 609, MAGNESIUM ION | | Authors: | Sabath, K, Jonas, S. | | Deposit date: | 2023-06-25 | | Release date: | 2024-07-03 | | Last modified: | 2024-07-24 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Basis of gene-specific transcription regulation by the Integrator complex.
Mol.Cell, 84, 2024
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7LA9
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7L9M
 | | Crystal structure of the first bromodomain (BD1) of human BRD4 in complex with bivalent inhibitor GXH-II-083 | | Descriptor: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, N,N'-[(1,19-dioxo-4,7,10,13,16-pentaoxanonadecane-1,19-diyl)di(piperidine-1,4-diyl)]bis(4-{[4-({3-[(tert-butylsulfonyl)amino]-4-chlorophenyl}amino)-5-methylpyrimidin-2-yl]amino}-2-fluorobenzamide) | | Authors: | Karim, M.R, Schonbrunn, E. | | Deposit date: | 2021-01-04 | | Release date: | 2022-01-12 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.45 Å) | | Cite: | Bivalent BET Bromodomain Inhibitors Confer Increased Potency and Selectivity for BRDT via Protein Conformational Plasticity.
J.Med.Chem., 65, 2022
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8PR7
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8PTT
 | | Human NUDT5 in complex with MRK-952 | | Descriptor: | 6-[(5~{R})-7-[3-chloranyl-4-(trifluoromethyl)phenyl]-2,7-diazaspiro[4.4]nonan-2-yl]-7-methyl-purine, ADP-sugar pyrophosphatase, MAGNESIUM ION | | Authors: | Diaz-Saez, L, Koekemoer, L, Feyerherm, C, Sloman, S, Fischer, C, Schneider, S, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Huber, K.V.M. | | Deposit date: | 2023-07-14 | | Release date: | 2024-07-24 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Human NUDT5 in complex with MRK-952
To Be Published
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7LNH
 | | S-adenosylmethionine synthetase co-crystallized with UppNHp | | Descriptor: | (2~{S})-2-azanyl-4-[[(2~{S},3~{S},4~{R},5~{R})-5-[2,4-bis(oxidanylidene)pyrimidin-1-yl]-3,4-bis(oxidanyl)oxolan-2-yl]methyl-methyl-$l^{3}-sulfanyl]butanoic acid, 1,2-ETHANEDIOL, S-adenosylmethionine synthase isoform type-2 | | Authors: | Tan, L.L, Jackson, C.J. | | Deposit date: | 2021-02-07 | | Release date: | 2022-03-02 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Substrate Dynamics Contribute to Enzymatic Specificity in Human and Bacterial Methionine Adenosyltransferases.
Jacs Au, 1, 2021
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8PJ2
 | | Structure of human 48S translation initiation complex in AUG recognition state after eIF5-induced GTP hydrolysis by eIF2 (48S-2) | | Descriptor: | 18S rRNA, 40S ribosomal protein S10, 40S ribosomal protein S11, ... | | Authors: | Petrychenko, V, Yi, S.-H, Liedtke, D, Peng, B.Z, Rodnina, M.V, Fischer, N. | | Deposit date: | 2023-06-22 | | Release date: | 2024-08-14 | | Last modified: | 2024-10-02 | | Method: | ELECTRON MICROSCOPY (3.4 Å) | | Cite: | Structural basis for translational control by the human 48S initiation complex.
Nat.Struct.Mol.Biol., 2024
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8PJ6
 | | Structure of human 48S translation initiation complex with initiator tRNA, eIF1A and eIF3 (off-pathway) | | Descriptor: | 18S rRNA, 40S ribosomal protein S10, 40S ribosomal protein S11, ... | | Authors: | Petrychenko, V, Yi, S.-H, Liedtke, D, Peng, B.Z, Rodnina, M.V, Fischer, N. | | Deposit date: | 2023-06-22 | | Release date: | 2024-08-14 | | Last modified: | 2024-10-02 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Structural basis for translational control by the human 48S initiation complex.
Nat.Struct.Mol.Biol., 2024
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8PJ4
 | | Structure of human 48S translation initiation complex after eIF5 release (48S-4) | | Descriptor: | 18S rRNA, 40S ribosomal protein S10, 40S ribosomal protein S11, ... | | Authors: | Petrychenko, V, Yi, S.-H, Liedtke, D, Peng, B.Z, Rodnina, M.V, Fischer, N. | | Deposit date: | 2023-06-22 | | Release date: | 2024-08-14 | | Last modified: | 2024-10-02 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Structural basis for translational control by the human 48S initiation complex.
Nat.Struct.Mol.Biol., 2024
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8PJ1
 | | Structure of human 48S translation initiation complex in open codon scanning state (48S-1) | | Descriptor: | 18S rRNA, 40S ribosomal protein S10, 40S ribosomal protein S11, ... | | Authors: | Petrychenko, V, Yi, S.-H, Liedtke, D, Peng, B.Z, Rodnina, M.V, Fischer, N. | | Deposit date: | 2023-06-22 | | Release date: | 2024-08-14 | | Last modified: | 2024-10-02 | | Method: | ELECTRON MICROSCOPY (3.4 Å) | | Cite: | Structural basis for translational control by the human 48S initiation complex.
Nat.Struct.Mol.Biol., 2024
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8PJ5
 | | Structure of human 48S translation initiation complex after eIF2 release prior 60S subunit joining (48S-5) | | Descriptor: | 18S rRNA, 40S ribosomal protein S10, 40S ribosomal protein S11, ... | | Authors: | Petrychenko, V, Yi, S.-H, Liedtke, D, Peng, B.Z, Rodnina, M.V, Fischer, N. | | Deposit date: | 2023-06-22 | | Release date: | 2024-08-14 | | Last modified: | 2024-10-02 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Structural basis for translational control by the human 48S initiation complex.
Nat.Struct.Mol.Biol., 2024
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8PJ3
 | | Structure of human 48S translation initiation complex upon transfer of initiator tRNA to eIF5B (48S-3) | | Descriptor: | 18S rRNA, 40S ribosomal protein S10, 40S ribosomal protein S11, ... | | Authors: | Petrychenko, V, Yi, S.-H, Liedtke, D, Peng, B.Z, Rodnina, M.V, Fischer, N. | | Deposit date: | 2023-06-22 | | Release date: | 2024-08-14 | | Last modified: | 2024-10-02 | | Method: | ELECTRON MICROSCOPY (3.7 Å) | | Cite: | Structural basis for translational control by the human 48S initiation complex.
Nat.Struct.Mol.Biol., 2024
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7M40
 | | Discovery of small molecule antagonists of human Retinoblastoma Binding Protein 4 (RBBP4) | | Descriptor: | Histone-binding protein RBBP4, N~3~-{4-[3-(dimethylamino)pyrrolidin-1-yl]-6,7-dimethoxyquinazolin-2-yl}-N~1~,N~1~-dimethylpropane-1,3-diamine | | Authors: | Perveen, S, Dong, A, Tempel, W, Zepeda-Velazquez, C, Abbey, M, McLeod, D, Marcellus, R, Mohammed, M, Ensan, D, Panagopoulos, D, Trush, V, Gibson, E, Brown, P.J, Arrowsmith, C.H, Schapira, M, Al-awar, R, Vedadi, M, Structural Genomics Consortium (SGC) | | Deposit date: | 2021-03-19 | | Release date: | 2021-05-12 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.88 Å) | | Cite: | Discovery of small molecule antagonists of human Retinoblastoma Binding Protein 4 (RBBP4)
To Be Published
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7MCF
 | | CRYSTAL STRUCTURE OF THE FIRST BROMODOMAIN OF HUMAN BRD4 IN COMPLEX WITH 2-{3-(1,4-dimethyl-1H-1,2,3-triazol-5-yl)-6-fluoro-5-[(S)-(3-fluoropyridin-2-yl)(oxan-4-yl)methyl]-5H-pyrido[3,2-b]indol-7-yl}propan-2-ol | | Descriptor: | 2-{3-(1,4-dimethyl-1H-1,2,3-triazol-5-yl)-6-fluoro-5-[(S)-(3-fluoropyridin-2-yl)(oxan-4-yl)methyl]-5H-pyrido[3,2-b]indol-7-yl}propan-2-ol, Bromodomain-containing protein 4 | | Authors: | Sheriff, S. | | Deposit date: | 2021-04-02 | | Release date: | 2021-05-26 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.19 Å) | | Cite: | Development of BET inhibitors as potential treatments for cancer: A search for structural diversity.
Bioorg.Med.Chem.Lett., 44, 2021
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8Q91
 | | Structure of the human 20S U5 snRNP core | | Descriptor: | 116 kDa U5 small nuclear ribonucleoprotein component, CD2 antigen cytoplasmic tail-binding protein 2, GUANOSINE-5'-TRIPHOSPHATE, ... | | Authors: | Schneider, S, Galej, W.P. | | Deposit date: | 2023-08-19 | | Release date: | 2024-03-27 | | Last modified: | 2024-05-29 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | Structure of the human 20S U5 snRNP.
Nat.Struct.Mol.Biol., 31, 2024
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8QEY
 | | Structure of human Asc1/CD98hc heteromeric amino acid transporter | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, 4F2 cell-surface antigen heavy chain, ... | | Authors: | Martinez-Molledo, M, Rullo-Tubau, J, Errasti-Murugarren, E, Palacin, M, Llorca, O. | | Deposit date: | 2023-09-01 | | Release date: | 2024-04-10 | | Last modified: | 2024-10-16 | | Method: | ELECTRON MICROSCOPY (4 Å) | | Cite: | Structure and mechanisms of transport of human Asc1/CD98hc amino acid transporter.
Nat Commun, 15, 2024
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7MHD
 | | Thioesterase Domain of Human Fatty Acid Synthase (FASN-TE) binding a competitive inhibitor SBP-7635 | | Descriptor: | Fatty acid synthase, N,N-diethyl-4-{2-[(2-fluorophenyl)methyl]-1,3-thiazol-4-yl}benzene-1-sulfonamide | | Authors: | Aleshin, A.E, Lambert, L, Liddington, R.C, Cosford, N. | | Deposit date: | 2021-04-15 | | Release date: | 2022-04-20 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.03 Å) | | Cite: | Thioesterase Domain of Human Fatty Acid Synthase (FASN-TE) binding a competitive inhibitor SBP-7635
To Be Published
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7MHE
 | | Thioesterase Domain of Human Fatty Acid Synthase (FASN-TE) binding a competitive inhibitor SBP-7957 | | Descriptor: | 1,2-ETHANEDIOL, 4-{4-[2-(4-fluorophenyl)-1,3-thiazol-4-yl]benzene-1-sulfonyl}morpholine, Fatty acid synthase | | Authors: | Aleshin, A.E, Lambert, L, Liddington, R.C, Cosford, N. | | Deposit date: | 2021-04-15 | | Release date: | 2022-04-20 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Thioesterase Domain of Human Fatty Acid Synthase (FASN-TE) binding a competitive inhibitor SBP-7635
To Be Published
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8Q7W
 | | Structure of the recycling U5 snRNP bound to chaperone CD2BP2 (State 3) | | Descriptor: | 116 kDa U5 small nuclear ribonucleoprotein component, CD2 antigen cytoplasmic tail-binding protein 2, GUANOSINE-5'-TRIPHOSPHATE, ... | | Authors: | Riabov Bassat, D, Plaschka, C, Vorlaender, M.K. | | Deposit date: | 2023-08-17 | | Release date: | 2024-04-17 | | Last modified: | 2024-05-29 | | Method: | ELECTRON MICROSCOPY (3.9 Å) | | Cite: | Structural basis of human U5 snRNP late biogenesis and recycling.
Nat.Struct.Mol.Biol., 31, 2024
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