2A19
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![BU of 2a19 by Molmil](/molmil-images/mine/2a19) | PKR kinase domain- eIF2alpha- AMP-PNP complex. | Descriptor: | Eukaryotic translation initiation factor 2 alpha subunit, Interferon-induced, double-stranded RNA-activated protein kinase, ... | Authors: | Dar, A.C, Dever, T.E, Sicheri, F. | Deposit date: | 2005-06-19 | Release date: | 2005-09-27 | Last modified: | 2023-08-23 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Higher-Order Substrate Recognition of eIF2alpha by the RNA-Dependent Protein Kinase PKR. Cell(Cambridge,Mass.), 122, 2005
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2A1A
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![BU of 2a1a by Molmil](/molmil-images/mine/2a1a) | PKR kinase domain-eIF2alpha Complex | Descriptor: | Eukaryotic translation initiation factor 2 alpha subunit, Interferon-induced, double-stranded RNA-activated protein kinase | Authors: | Dar, A.C, Dever, T.E, Sicheri, F. | Deposit date: | 2005-06-19 | Release date: | 2005-09-27 | Last modified: | 2023-08-23 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Higher-Order Substrate Recognition of eIF2alpha by the RNA-Dependent Protein Kinase PKR. Cell(Cambridge,Mass.), 122, 2005
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3EL8
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![BU of 3el8 by Molmil](/molmil-images/mine/3el8) | Crystal structure of c-Src in complex with pyrazolopyrimidine 5 | Descriptor: | 1-{4-[4-amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]phenyl}-3-[3-(trifluoromethyl)phenyl]urea, Proto-oncogene tyrosine-protein kinase Src | Authors: | Dar, A.C, Lopez, M.S, Shokat, K.M. | Deposit date: | 2008-09-20 | Release date: | 2008-10-28 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Small molecule recognition of c-Src via the Imatinib-binding conformation. Chem.Biol., 15, 2008
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3EL7
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![BU of 3el7 by Molmil](/molmil-images/mine/3el7) | Crystal structure of c-Src in complex with pyrazolopyrimidine 3 | Descriptor: | 1-{3-[(4-amino-1-cyclopentyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)methyl]phenyl}-3-[3-(trifluoromethyl)phenyl]urea, Proto-oncogene tyrosine-protein kinase Src | Authors: | Dar, A.C, Lopez, M.S, Shokat, K.M. | Deposit date: | 2008-09-20 | Release date: | 2008-10-28 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Small molecule recognition of c-Src via the Imatinib-binding conformation. Chem.Biol., 15, 2008
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1LUZ
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![BU of 1luz by Molmil](/molmil-images/mine/1luz) | |
7UMB
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![BU of 7umb by Molmil](/molmil-images/mine/7umb) | NanoBRET tracer Tram-bo bound to a KSR2-MEK1 complex | Descriptor: | Dual specificity mitogen-activated protein kinase kinase 1, Kinase suppressor of Ras 2, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | Authors: | Marsiglia, W.M, Khan, K.M, Dar, A.C. | Deposit date: | 2022-04-06 | Release date: | 2023-09-27 | Last modified: | 2024-03-20 | Method: | X-RAY DIFFRACTION (3.231 Å) | Cite: | Live-cell target engagement of allosteric MEKi on MEK-RAF/KSR-14-3-3 complexes. Nat.Chem.Biol., 20, 2024
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4LGG
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![BU of 4lgg by Molmil](/molmil-images/mine/4lgg) | Structure of 3MB-PP1 bound to analog-sensitive Src kinase | Descriptor: | 1-tert-butyl-3-(3-methylbenzyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Proto-oncogene tyrosine-protein kinase Src | Authors: | Lopez, M.S, Dar, A.C, Shokat, K.M. | Deposit date: | 2013-06-27 | Release date: | 2013-08-07 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.41 Å) | Cite: | Structure-guided inhibitor design expands the scope of analog-sensitive kinase technology. Acs Chem.Biol., 8, 2013
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4LGH
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![BU of 4lgh by Molmil](/molmil-images/mine/4lgh) | |
7JUT
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![BU of 7jut by Molmil](/molmil-images/mine/7jut) | |
7JUQ
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![BU of 7juq by Molmil](/molmil-images/mine/7juq) | Crystal Structure of KSR2:MEK1 in complex with ADP | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, Dual specificity mitogen-activated protein kinase kinase 1, Kinase suppressor of Ras 2, ... | Authors: | Khan, Z.M, Dar, A.C. | Deposit date: | 2020-08-20 | Release date: | 2020-09-30 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (3.22 Å) | Cite: | Structural basis for the action of the drug trametinib at KSR-bound MEK. Nature, 588, 2020
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7JUR
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![BU of 7jur by Molmil](/molmil-images/mine/7jur) | |
7JUX
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![BU of 7jux by Molmil](/molmil-images/mine/7jux) | |
7JUS
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![BU of 7jus by Molmil](/molmil-images/mine/7jus) | |
7JV0
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![BU of 7jv0 by Molmil](/molmil-images/mine/7jv0) | |
7JUW
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![BU of 7juw by Molmil](/molmil-images/mine/7juw) | Crystal Structure of KSR1:MEK1 in complex with AMP-PNP | Descriptor: | Dual specificity mitogen-activated protein kinase kinase 1, Kinase suppressor of Ras 1, MAGNESIUM ION, ... | Authors: | Khan, Z.M, Dar, A.C. | Deposit date: | 2020-08-20 | Release date: | 2020-09-30 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.88 Å) | Cite: | Structural basis for the action of the drug trametinib at KSR-bound MEK. Nature, 588, 2020
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7JV1
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![BU of 7jv1 by Molmil](/molmil-images/mine/7jv1) | Crystal Structure of KSR1:MEK1 in complex with AMP-PNP, and allosteric MEK inhibitor APS-9-95-1 | Descriptor: | Dual specificity mitogen-activated protein kinase kinase 1, Kinase suppressor of Ras 1, MAGNESIUM ION, ... | Authors: | Khan, Z.M, Dar, A.C, Scopton, A.P. | Deposit date: | 2020-08-20 | Release date: | 2020-09-30 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (3.62 Å) | Cite: | Structural basis for the action of the drug trametinib at KSR-bound MEK. Nature, 588, 2020
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7JUV
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![BU of 7juv by Molmil](/molmil-images/mine/7juv) | Crystal Structure of KSR2:MEK1 in complex with AMP-PNP, and allosteric MEK inhibitor APS-9-95-1 | Descriptor: | Dual specificity mitogen-activated protein kinase kinase 1, Kinase suppressor of Ras 2, MAGNESIUM ION, ... | Authors: | Khan, Z.M, Dar, A.C, Scopton, A.P. | Deposit date: | 2020-08-20 | Release date: | 2020-09-30 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (3.36 Å) | Cite: | Structural basis for the action of the drug trametinib at KSR-bound MEK. Nature, 588, 2020
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7JUU
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![BU of 7juu by Molmil](/molmil-images/mine/7juu) | |
7JUZ
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![BU of 7juz by Molmil](/molmil-images/mine/7juz) | |
7JUY
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![BU of 7juy by Molmil](/molmil-images/mine/7juy) | |
5KKR
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![BU of 5kkr by Molmil](/molmil-images/mine/5kkr) | KSR2:MEK1 Complex Bound to the Small Molecule APS-2-79 | Descriptor: | 6,7-dimethoxy-~{N}-(2-methyl-4-phenoxy-phenyl)quinazolin-4-amine, Dual specificity mitogen-activated protein kinase kinase 1, Kinase suppressor of Ras 2 | Authors: | Dhawan, N.S, Scopton, A.P, Dar, A.C. | Deposit date: | 2016-06-22 | Release date: | 2016-08-31 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (3.509 Å) | Cite: | Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature, 537, 2016
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2Y4I
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![BU of 2y4i by Molmil](/molmil-images/mine/2y4i) | KSR2-MEK1 heterodimer | Descriptor: | ADENOSINE-5'-TRIPHOSPHATE, CHLORIDE ION, DUAL SPECIFICITY MITOGEN-ACTIVATED PROTEIN KINASE KINASE 1, ... | Authors: | Brennan, D.F, Barford, D. | Deposit date: | 2011-01-06 | Release date: | 2011-01-19 | Last modified: | 2023-12-20 | Method: | X-RAY DIFFRACTION (3.46 Å) | Cite: | A Raf-Induced Allosteric Transition of Ksr Stimulates Ksr and Raf Phosphorylation of Mek Nature, 472, 2011
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9AXC
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![BU of 9axc by Molmil](/molmil-images/mine/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 | Last modified: | 2024-07-10 | Method: | ELECTRON MICROSCOPY (4.16 Å) | Cite: | The Pan-RAF-MEK Nondegrading 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, 14, 2024
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9AXM
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![BU of 9axm by Molmil](/molmil-images/mine/9axm) | Crystal structure of ARAF/MEK1 complex with NST-628 and a RAF dimer | Descriptor: | 1,2-ETHANEDIOL, Dual specificity mitogen-activated protein kinase kinase 1, GLYCEROL, ... | Authors: | Quade, B, Huang, X. | Deposit date: | 2024-03-06 | Release date: | 2024-04-17 | Last modified: | 2024-07-10 | Method: | X-RAY DIFFRACTION (2.42 Å) | Cite: | The Pan-RAF-MEK Nondegrading 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, 14, 2024
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9AXX
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![BU of 9axx by Molmil](/molmil-images/mine/9axx) | Crystal structure of BRAF/MEK1 complex with NST-628 and an active RAF dimer | Descriptor: | 1,2-ETHANEDIOL, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, Dual specificity mitogen-activated protein kinase kinase 1, ... | Authors: | Quade, B, Huang, X. | Deposit date: | 2024-03-06 | Release date: | 2024-04-17 | Last modified: | 2024-07-10 | Method: | X-RAY DIFFRACTION (2.07 Å) | Cite: | The Pan-RAF-MEK Nondegrading 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, 14, 2024
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