6XMX
| Cryo-EM structure of BCL6 bound to BI-3802 | Descriptor: | 2-[6-[[5-chloranyl-2-[(3~{S},5~{R})-3,5-dimethylpiperidin-1-yl]pyrimidin-4-yl]amino]-1-methyl-2-oxidanylidene-quinolin-3-yl]oxy-~{N}-methyl-ethanamide, B-cell lymphoma 6 protein | Authors: | Yoon, H, Burman, S.S.R, Hunkeler, M, Nowak, R.P, Fischer, E.S. | Deposit date: | 2020-07-01 | Release date: | 2020-11-25 | Last modified: | 2024-03-06 | Method: | ELECTRON MICROSCOPY (3.7 Å) | Cite: | Small-molecule-induced polymerization triggers degradation of BCL6. Nature, 588, 2020
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7UP7
| Crystal structure of C-terminal Domain of MSK1 in complex with covalently bound with literature RSK2 inhibitor indazole cyanoacrylamide compound 26 (soak) | Descriptor: | (2S)-2-cyano-N-(1-hydroxy-2-methylpropan-2-yl)-3-[3-(3,4,5-trimethoxyphenyl)-1H-indazol-5-yl]propanamide, Ribosomal protein S6 kinase alpha-5 | Authors: | Yano, J.K, Abendroth, J, Hall, A. | Deposit date: | 2022-04-14 | Release date: | 2022-07-20 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Discovery and Characterization of a Novel Series of Chloropyrimidines as Covalent Inhibitors of the Kinase MSK1. Acs Med.Chem.Lett., 13, 2022
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7UP6
| Crystal structure of C-terminal domain of MSK1 in complex with in covalently bound literature RSK2 inhibitor pyrrolopyrimidine cyanoacrylamide compound 25 (co-crystal) | Descriptor: | (E)-3-(3-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)-2-cyanoacrylamide bound form, OXAMIC ACID, Ribosomal protein S6 kinase alpha-5 | Authors: | Yano, J.K, Abendroth, J, Hall, A. | Deposit date: | 2022-04-14 | Release date: | 2022-08-31 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (2.6 Å) | Cite: | Discovery and Characterization of a Novel Series of Chloropyrimidines as Covalent Inhibitors of the Kinase MSK1. Acs Med.Chem.Lett., 13, 2022
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7UP4
| Crystal structure of C-terminal Domain of MSK1 in complex with covalently bound pyrrolopyrimidine compound 20 (co-crystal) | Descriptor: | (5M)-5-(2,5-dichloropyrimidin-4-yl)-5H-pyrrolo[3,2-d]pyrimidine, Ribosomal protein S6 kinase alpha-5 | Authors: | Yano, J.K, Abendroth, J, Hall, A. | Deposit date: | 2022-04-14 | Release date: | 2022-07-06 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (3 Å) | Cite: | Discovery and Characterization of a Novel Series of Chloropyrimidines as Covalent Inhibitors of the Kinase MSK1. Acs Med.Chem.Lett., 13, 2022
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7UP8
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7UP5
| Crystal structure of C-terminal Domain of MSK1 in complex with covalently bound pyrrolopyrimidine compound 23 (co-crystal) | Descriptor: | (2M)-6-chloro-2-(5H-pyrrolo[3,2-d]pyrimidin-5-yl)pyridine-3-carbonitrile, IODIDE ION, Ribosomal protein S6 kinase alpha-5 | Authors: | Yano, J.K, Edwards, T.E, Hall, A. | Deposit date: | 2022-04-14 | Release date: | 2022-07-06 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Discovery and Characterization of a Novel Series of Chloropyrimidines as Covalent Inhibitors of the Kinase MSK1. Acs Med.Chem.Lett., 13, 2022
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7Z38
| Structure of the RAF1-HSP90-CDC37 complex (RHC-I) | Descriptor: | ADENOSINE-5'-TRIPHOSPHATE, Heat shock protein HSP 90-beta, Hsp90 co-chaperone Cdc37, ... | Authors: | Mesa, P, Garcia-Alonso, S, Barbacid, M, Montoya, G. | Deposit date: | 2022-03-01 | Release date: | 2022-09-14 | Last modified: | 2022-09-28 | Method: | ELECTRON MICROSCOPY (3.16 Å) | Cite: | Structure of the RAF1-HSP90-CDC37 complex reveals the basis of RAF1 regulation. Mol.Cell, 82, 2022
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7Z37
| Structure of the RAF1-HSP90-CDC37 complex (RHC-II) | Descriptor: | ADENOSINE-5'-TRIPHOSPHATE, Heat shock protein HSP 90-beta, Hsp90 co-chaperone Cdc37, ... | Authors: | Mesa, P, Garcia-Alonso, S, Barbacid, M, Montoya, G. | Deposit date: | 2022-03-01 | Release date: | 2022-09-14 | Last modified: | 2022-09-28 | Method: | ELECTRON MICROSCOPY (3.67 Å) | Cite: | Structure of the RAF1-HSP90-CDC37 complex reveals the basis of RAF1 regulation. Mol.Cell, 82, 2022
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3KN6
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6NYB
| Structure of a MAPK pathway complex | Descriptor: | 14-3-3 protein zeta, 5-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)imidazo[1,5-a]pyridine-6-carboxamide, ADENOSINE-5'-DIPHOSPHATE, ... | Authors: | Park, E, Rawson, S, Li, K, Jeon, H, Eck, M.J. | Deposit date: | 2019-02-11 | Release date: | 2019-10-09 | Last modified: | 2020-04-22 | Method: | ELECTRON MICROSCOPY (4.1 Å) | Cite: | Architecture of autoinhibited and active BRAF-MEK1-14-3-3 complexes. Nature, 575, 2019
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7W4P
| The structure of KATP H175K mutant in closed state | Descriptor: | 6-chloranyl-~{N}-(1-methylcyclopropyl)-1,1-bis(oxidanylidene)-4~{H}-thieno[3,2-e][1,2,4]thiadiazin-3-amine, ADENOSINE-5'-DIPHOSPHATE, ADENOSINE-5'-TRIPHOSPHATE, ... | Authors: | Chen, L, Wang, M. | Deposit date: | 2021-11-28 | Release date: | 2022-06-01 | Method: | ELECTRON MICROSCOPY (3.19 Å) | Cite: | Structural insights into the mechanism of pancreatic K ATP channel regulation by nucleotides. Nat Commun, 13, 2022
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7W4O
| The structure of KATP H175K mutant in pre-open state | Descriptor: | 6-chloranyl-~{N}-(1-methylcyclopropyl)-1,1-bis(oxidanylidene)-4~{H}-thieno[3,2-e][1,2,4]thiadiazin-3-amine, ADENOSINE-5'-DIPHOSPHATE, ADENOSINE-5'-TRIPHOSPHATE, ... | Authors: | Chen, L, Wang, M. | Deposit date: | 2021-11-28 | Release date: | 2022-06-01 | Method: | ELECTRON MICROSCOPY (2.96 Å) | Cite: | Structural insights into the mechanism of pancreatic K ATP channel regulation by nucleotides. Nat Commun, 13, 2022
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8TI1
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9AXC
| Activated CRAF/MEK heterotetramer from focused refinement of CRAF/MEK/14-3-3 complex | Descriptor: | Dual specificity mitogen-activated protein kinase kinase 1, GST26/CRAF chimera, N-[3-fluoro-4-({7-[(3-fluoropyridin-2-yl)oxy]-4-methyl-2-oxo-2H-1-benzopyran-3-yl}methyl)pyridin-2-yl]-N'-methylsulfuric diamide | Authors: | Quade, B, Cohen, S.E, Huang, X. | Deposit date: | 2024-03-06 | Release date: | 2024-04-17 | Method: | ELECTRON MICROSCOPY (4.16 Å) | Cite: | The pan-RAF-MEK non degrading molecular glue NST-628 is a potent and brain penetrant inhibitor of the RAS-MAPK pathway with activity across diverse RAS- and RAF-driven cancers. Cancer Discov, 2024
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8TI2
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9AXA
| CryoEM structure of activated CRAF/MEK/14-3-3 complex with NST-628 | Descriptor: | 14-3-3 protein sigma, Dual specificity mitogen-activated protein kinase kinase 1, GST26/CRAF chimera, ... | Authors: | Quade, B, Cohen, S.E, Huang, X. | Deposit date: | 2024-03-06 | Release date: | 2024-04-17 | Method: | ELECTRON MICROSCOPY (4.36 Å) | Cite: | The pan-RAF-MEK non degrading molecular glue NST-628 is a potent and brain penetrant inhibitor of the RAS-MAPK pathway with activity across diverse RAS- and RAF-driven cancers. Cancer Discov, 2024
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7S5X
| Human KATP channel in open conformation, focused on Kir and one SUR, position 1 | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, ADENOSINE-5'-TRIPHOSPHATE, ATP-binding cassette sub-family C member 8, ... | Authors: | Zhao, C, MacKinnon, R. | Deposit date: | 2021-09-12 | Release date: | 2021-12-01 | Last modified: | 2021-12-08 | Method: | ELECTRON MICROSCOPY (3.7 Å) | Cite: | Molecular structure of an open human K ATP channel. Proc.Natl.Acad.Sci.USA, 118, 2021
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7S5Y
| Human KATP channel in open conformation, focused on Kir and one SUR, position 2 | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, ADENOSINE-5'-TRIPHOSPHATE, ATP-binding cassette sub-family C member 8, ... | Authors: | Zhao, C, MacKinnon, R. | Deposit date: | 2021-09-12 | Release date: | 2021-12-01 | Last modified: | 2021-12-08 | Method: | ELECTRON MICROSCOPY (3.9 Å) | Cite: | Molecular structure of an open human K ATP channel. Proc.Natl.Acad.Sci.USA, 118, 2021
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7S5T
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7S61
| Human KATP channel in open conformation, focused on Kir and one SUR, position 5 | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, ADENOSINE-5'-TRIPHOSPHATE, ATP-binding cassette sub-family C member 8, ... | Authors: | Zhao, C, MacKinnon, R. | Deposit date: | 2021-09-12 | Release date: | 2021-12-01 | Last modified: | 2021-12-08 | Method: | ELECTRON MICROSCOPY (4 Å) | Cite: | Molecular structure of an open human K ATP channel. Proc.Natl.Acad.Sci.USA, 118, 2021
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7S5Z
| Human KATP channel in open conformation, focused on Kir and one SUR, position 3 | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, ADENOSINE-5'-TRIPHOSPHATE, ATP-binding cassette sub-family C member 8, ... | Authors: | Zhao, C, MacKinnon, R. | Deposit date: | 2021-09-12 | Release date: | 2021-12-01 | Last modified: | 2021-12-08 | Method: | ELECTRON MICROSCOPY (3.9 Å) | Cite: | Molecular structure of an open human K ATP channel. Proc.Natl.Acad.Sci.USA, 118, 2021
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7S60
| Human KATP channel in open conformation, focused on Kir and one SUR, position 4 | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, ADENOSINE-5'-TRIPHOSPHATE, ATP-binding cassette sub-family C member 8, ... | Authors: | Zhao, C, MacKinnon, R. | Deposit date: | 2021-09-12 | Release date: | 2021-12-01 | Last modified: | 2021-12-08 | Method: | ELECTRON MICROSCOPY (3.7 Å) | Cite: | Molecular structure of an open human K ATP channel. Proc.Natl.Acad.Sci.USA, 118, 2021
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7MFD
| Autoinhibited BRAF:(14-3-3)2:MEK complex with the BRAF RBD resolved | Descriptor: | 14-3-3 protein zeta/delta, Dual specificity mitogen-activated protein kinase kinase 1, N-(3-fluoro-4-{[4-methyl-2-oxo-7-(pyrimidin-2-yloxy)-2H-chromen-3-yl]methyl}pyridin-2-yl)-N'-methylsulfuric diamide, ... | Authors: | Martinez Fiesco, J.A, Ping, Z, Durrant, D.E, Morrison, D.K. | Deposit date: | 2021-04-09 | Release date: | 2022-01-26 | Last modified: | 2022-02-09 | Method: | ELECTRON MICROSCOPY (3.66 Å) | Cite: | Structural insights into the BRAF monomer-to-dimer transition mediated by RAS binding. Nat Commun, 13, 2022
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8DGT
| Cryo-EM structure of a RAS/RAF complex (state 2) | Descriptor: | 14-3-3 protein zeta, 5-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)imidazo[1,5-a]pyridine-6-carboxamide, Dual specificity mitogen-activated protein kinase kinase 1, ... | Authors: | Eck, M.J, Jeon, H, Park, E, Rawson, S. | Deposit date: | 2022-06-24 | Release date: | 2023-07-05 | Last modified: | 2023-08-09 | Method: | ELECTRON MICROSCOPY (3.9 Å) | Cite: | Cryo-EM structure of a RAS/RAF recruitment complex. Nat Commun, 14, 2023
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8DGS
| Cryo-EM structure of a RAS/RAF complex (state 1) | Descriptor: | 14-3-3 protein zeta, 5-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)imidazo[1,5-a]pyridine-6-carboxamide, Dual specificity mitogen-activated protein kinase kinase 1, ... | Authors: | Eck, M.J, Jeon, H, Park, E, Rawson, S. | Deposit date: | 2022-06-24 | Release date: | 2023-07-05 | Last modified: | 2023-08-09 | Method: | ELECTRON MICROSCOPY (4.3 Å) | Cite: | Cryo-EM structure of a RAS/RAF recruitment complex. Nat Commun, 14, 2023
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