8CTB
| Human PRMT5:MEP50 structure with Fragment 3 and MTA Bound | Descriptor: | 5'-DEOXY-5'-METHYLTHIOADENOSINE, 7-chloro-1-methyl-1H-benzimidazol-2-amine, Methylosome protein 50, ... | Authors: | Gunn, R.J, Lawson, J.D, Smith, C.R. | Deposit date: | 2022-05-13 | Release date: | 2022-10-05 | Last modified: | 2023-10-25 | Method: | X-RAY DIFFRACTION (2.61 Å) | Cite: | Fragment optimization and elaboration strategies - the discovery of two lead series of PRMT5/MTA inhibitors from five fragment hits. Rsc Med Chem, 13, 2022
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8CTI
| Cryo-EM structure of human METTL1-WDR4-tRNA(Val) complex | Descriptor: | tRNA (guanine-N(7)-)-methyltransferase, tRNA (guanine-N(7)-)-methyltransferase non-catalytic subunit WDR4, tRNA-Val-TAC-2-1 | Authors: | Li, J, Wang, L, Fontana, P, Hunkeler, M, Roy-Burman, S.S, Wu, H, Fischer, E.S, Gregory, R.I. | Deposit date: | 2022-05-14 | Release date: | 2022-12-07 | Last modified: | 2023-01-25 | Method: | ELECTRON MICROSCOPY (3.6 Å) | Cite: | Structural basis of regulated m 7 G tRNA modification by METTL1-WDR4. Nature, 613, 2023
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8CTH
| Cryo-EM structure of human METTL1-WDR4-tRNA(Phe) complex | Descriptor: | Phe-tRNA, S-ADENOSYL-L-HOMOCYSTEINE, tRNA (guanine-N(7)-)-methyltransferase, ... | Authors: | Li, J, Wang, L, Fontana, P, Hunkeler, M, Roy-Burman, S.S, Wu, H, Fishcer, E.S, Gregory, R.I. | Deposit date: | 2022-05-14 | Release date: | 2022-12-07 | Last modified: | 2023-01-25 | Method: | ELECTRON MICROSCOPY (3.3 Å) | Cite: | Structural basis of regulated m 7 G tRNA modification by METTL1-WDR4. Nature, 613, 2023
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7PQH
| Cryo-EM structure of Saccharomyces cerevisiae TOROID (TORC1 Organized in Inhibited Domains). | Descriptor: | Serine/threonine-protein kinase TOR2, Target of rapamycin complex 1 subunit KOG1,Target of rapamycin complex 1 subunit Kog1, Target of rapamycin complex subunit LST8 | Authors: | Felix, J, Prouteau, M, Bourgoint, C, Bonadei, L, Desfosses, A, Gabus, C, Sadian, Y, Savvides, S.N, Gutsche, I, Loewith, R. | Deposit date: | 2021-09-17 | Release date: | 2023-01-18 | Last modified: | 2023-03-29 | Method: | ELECTRON MICROSCOPY (3.87 Å) | Cite: | EGOC inhibits TOROID polymerization by structurally activating TORC1. Nat.Struct.Mol.Biol., 30, 2023
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7R1D
| Structure of MuvB complex | Descriptor: | Histone-binding protein RBBP4, Protein lin-37 homolog, Protein lin-9 homolog | Authors: | Koliopoulos, M.G, Alfieri, C. | Deposit date: | 2022-02-02 | Release date: | 2022-08-10 | Last modified: | 2022-09-14 | Method: | ELECTRON MICROSCOPY (3.5 Å) | Cite: | Structure of a nucleosome-bound MuvB transcription factor complex reveals DNA remodelling. Nat Commun, 13, 2022
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7QE7
| High-resolution structure of the Anaphase-promoting complex/cyclosome (APC/C) bound to co-activator Cdh1 | Descriptor: | Anaphase-promoting complex subunit 1, Anaphase-promoting complex subunit 10, Anaphase-promoting complex subunit 11, ... | Authors: | Hoefler, A, Yu, J, Chang, L, Zhang, Z, Yang, J, Boland, A, Barford, D. | Deposit date: | 2021-12-01 | Release date: | 2022-01-26 | Last modified: | 2024-05-22 | Method: | ELECTRON MICROSCOPY (2.9 Å) | Cite: | High-resolution structure of the Anaphase-promoting complex (APC/C) bound to co-activator Cdh1 To Be Published
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7QK4
| EED in complex with PRC2 allosteric inhibitor compound 22 (MAK683) | Descriptor: | CHLORIDE ION, Histone-lysine N-methyltransferase EZH2, N-[(5-fluoranyl-2,3-dihydro-1-benzofuran-4-yl)methyl]-8-(2-methylpyridin-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine, ... | Authors: | Zhao, K, Zhao, M, Luo, X, Zhang, H, Scheufler, C. | Deposit date: | 2021-12-17 | Release date: | 2022-04-13 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (1.602 Å) | Cite: | Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies. J.Med.Chem., 65, 2022
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7QJG
| EED in complex with PRC2 allosteric inhibitor compound 6 | Descriptor: | CHLORIDE ION, Histone-lysine N-methyltransferase EZH2, N-(2,3-dihydro-1-benzofuran-7-ylmethyl)-8-[4-[(dimethylamino)methyl]phenyl]-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine, ... | Authors: | Zhao, K, Zhao, M, Luo, X, Zhang, H, Scheufler, C. | Deposit date: | 2021-12-16 | Release date: | 2022-04-13 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies. J.Med.Chem., 65, 2022
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7QJU
| EED in complex with PRC2 allosteric inhibitor compound 7 | Descriptor: | CHLORIDE ION, Histone-lysine N-methyltransferase EZH2, N-(2,3-dihydro-1-benzofuran-4-ylmethyl)-8-[4-[(dimethylamino)methyl]phenyl]-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine, ... | Authors: | Zhao, K, Zhao, M, Luo, X, Zhang, H, Scheufler, C. | Deposit date: | 2021-12-17 | Release date: | 2022-04-13 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies. J.Med.Chem., 65, 2022
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8DDW
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8DDX
| cryo-EM structure of TRPM3 ion channel in complex with Gbg in the presence of PIP2, tethered by ALFA-nanobody | Descriptor: | (3beta,14beta,17beta,25R)-3-[4-methoxy-3-(methoxymethyl)butoxy]spirost-5-en, 1,2-DIACYL-GLYCEROL-3-SN-PHOSPHATE, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Zhao, C, MacKinnon, R. | Deposit date: | 2022-06-19 | Release date: | 2022-11-02 | Last modified: | 2023-01-18 | Method: | ELECTRON MICROSCOPY (3.8 Å) | Cite: | Structural and functional analyses of a GPCR-inhibited ion channel TRPM3. Neuron, 111, 2023
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8D30
| Crystal structure of the human COPB2 WD-domains | Descriptor: | 1,2-ETHANEDIOL, Coatomer subunit beta' | Authors: | Zeng, H, Dong, A, Hutchinson, A, Seitova, A, Loppnau, P, Arrowsmith, C.H, Edwards, A.M, Halabelian, L, Structural Genomics Consortium (SGC) | Deposit date: | 2022-05-31 | Release date: | 2022-11-16 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | Crystal structure of the human COPB2 WD-domains To Be Published
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8D9K
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8D58
| Crystal structure of human METTL1-WDR4 complex | Descriptor: | CHLORIDE ION, GLYCEROL, ISOPROPYL ALCOHOL, ... | Authors: | Raj, R, Babu, K, Nam, Y. | Deposit date: | 2022-06-04 | Release date: | 2023-01-11 | Last modified: | 2023-10-25 | Method: | X-RAY DIFFRACTION (2.47 Å) | Cite: | Structures and mechanisms of tRNA methylation by METTL1-WDR4. Nature, 613, 2023
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8D9L
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8CYI
| Cryo-EM structures and computational analysis for enhanced potency in MTA-synergic inhibition of human protein arginine methyltransferase 5 | Descriptor: | 5'-DEOXY-5'-METHYLTHIOADENOSINE, Methylosome protein 50, N-[(2-aminoquinolin-7-yl)methyl]-9-(2-hydroxyethyl)-2,3,4,9-tetrahydro-1H-carbazole-6-carboxamide, ... | Authors: | Yadav, G.P, Wei, Z, Xiaozhi, Y, Chenglong, L, Jiang, Q. | Deposit date: | 2022-05-23 | Release date: | 2023-04-12 | Method: | ELECTRON MICROSCOPY (3.14 Å) | Cite: | Cryo-EM structure-based selection of computed ligand poses enables design of MTA-synergic PRMT5 inhibitors of better potency. Commun Biol, 5, 2022
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7R6K
| State E2 nucleolar 60S ribosomal intermediate - Model for Noc2/Noc3 region | Descriptor: | 25S rRNA, 25S rRNA (cytosine(2870)-C(5))-methyltransferase, 27S pre-rRNA (guanosine(2922)-2'-O)-methyltransferase, ... | Authors: | Cruz, V.E, Sekulski, K, Peddada, N, Erzberger, J.P. | Deposit date: | 2021-06-22 | Release date: | 2022-11-09 | Last modified: | 2022-12-28 | Method: | ELECTRON MICROSCOPY (3.17 Å) | Cite: | Sequence-specific remodeling of a topologically complex RNP substrate by Spb4. Nat.Struct.Mol.Biol., 29, 2022
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8EG0
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8DYV
| Structure of human cytoplasmic dynein-1 bound to one Lis1 | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, ADENOSINE-5'-TRIPHOSPHATE, Cytoplasmic dynein 1 heavy chain 1, ... | Authors: | Reimer, J.M, DeSantis, M, Reck-Peterson, S.L, Leschziner, A.E. | Deposit date: | 2022-08-05 | Release date: | 2023-02-01 | Method: | ELECTRON MICROSCOPY (3.97 Å) | Cite: | Structures of human dynein in complex with the lissencephaly 1 protein, LIS1. Elife, 12, 2023
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8DYU
| Structure of human cytoplasmic dynein-1 bound to two Lis1 proteins | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, ADENOSINE-5'-TRIPHOSPHATE, Cytoplasmic dynein 1 heavy chain 1, ... | Authors: | Reimer, J.M, DeSantis, M, Reck-Peterson, S.L, Leschziner, A.E. | Deposit date: | 2022-08-05 | Release date: | 2023-02-01 | Method: | ELECTRON MICROSCOPY (4 Å) | Cite: | Structures of human dynein in complex with the lissencephaly 1 protein, LIS1. Elife, 12, 2023
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7S1Q
| PRMT5/MEP50 crystal structure with MTA and a phthalazinone inhibitor bound (Compound 9) | Descriptor: | 5'-DEOXY-5'-METHYLTHIOADENOSINE, Methylosome protein 50, Protein arginine N-methyltransferase 5, ... | Authors: | Gunn, R.J, Thomas, N.C, Lawson, J.D, Ivetac, A, Smith, C.R, Kulyk, S, Marx, M.A. | Deposit date: | 2021-09-02 | Release date: | 2022-01-26 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.78 Å) | Cite: | Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP -Deleted Cancers. J.Med.Chem., 65, 2022
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7S1S
| PRMT5/MEP50 crystal structure with MTA and MRTX-1719 bound | Descriptor: | (7-{(5M)-5-[3-chloro-6-cyano-5-(cyclopropyloxy)-2-fluorophenyl]-1-methyl-1H-pyrazol-4-yl}-4-oxo-3,4-dihydrophthalazin-1-yl)methanaminium, 5'-DEOXY-5'-METHYLTHIOADENOSINE, Methylosome protein 50, ... | Authors: | Gunn, R.J, Thomas, N.C, Lawson, J.D, Ivetac, A, Kulyk, S, Smith, C.R, Marx, M.A. | Deposit date: | 2021-09-02 | Release date: | 2022-01-26 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.62 Å) | Cite: | Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP -Deleted Cancers. J.Med.Chem., 65, 2022
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7SES
| PRMT5/MEP50 with compound 29 bound | Descriptor: | (2P)-2-{4-[4-(aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl]-1-methyl-1H-pyrazol-5-yl}naphthalene-1-carbonitrile, 5'-DEOXY-5'-METHYLTHIOADENOSINE, Methylosome protein 50, ... | Authors: | Gunn, R.J, Thomas, N.C, Lawson, J.D, Ivetac, A, Smith, C.R, Kulyk, S, Marx, M.A. | Deposit date: | 2021-10-01 | Release date: | 2022-01-26 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP -Deleted Cancers. J.Med.Chem., 65, 2022
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7S1R
| PRMT5/MEP50 crystal structure with MTA and a phthalazinone inhibitor bound (compound (M)-31) | Descriptor: | 5'-DEOXY-5'-METHYLTHIOADENOSINE, Methylosome protein 50, Protein arginine N-methyltransferase 5, ... | Authors: | Gunn, R.J, Thomas, N.C, Lawson, J.D, Ivetac, A, Kulyk, S, Smith, C.R, Marx, M.A. | Deposit date: | 2021-09-02 | Release date: | 2022-01-26 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP -Deleted Cancers. J.Med.Chem., 65, 2022
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7SER
| PRMT5/MEP50 with compound 30 bound | Descriptor: | (2M)-2-{4-[4-(aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl]-1-methyl-1H-pyrazol-5-yl}-1-benzothiophene-3-carbonitrile, 5'-DEOXY-5'-METHYLTHIOADENOSINE, Methylosome protein 50, ... | Authors: | Gunn, R.J, Thomas, N.C, Lawson, J.D, Ivetac, A, Smith, C.R, Kulyk, S, Marx, M.A. | Deposit date: | 2021-10-01 | Release date: | 2022-01-26 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.14 Å) | Cite: | Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP -Deleted Cancers. J.Med.Chem., 65, 2022
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