7M0Z
 
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and CH5126766 | | 分子名称: | Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, N-(3-fluoro-4-{[4-methyl-2-oxo-7-(pyrimidin-2-yloxy)-2H-chromen-3-yl]methyl}pyridin-2-yl)-N'-methylsulfuric diamide, ... | | 著者 | Li, K, Gonzalez Del-Pino, G, Ha, B.H, Park, E, Eck, M.J. | | 登録日 | 2021-03-11 | | 公開日 | 2021-04-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.12 Å) | | 主引用文献 | Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7M0Y
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Trametinib | | 分子名称: | Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | 著者 | Li, K, Gonzalez Del-Pino, G, Ha, B.H, Park, E, Eck, M.J. | | 登録日 | 2021-03-11 | | 公開日 | 2021-04-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.45 Å) | | 主引用文献 | Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7M0X
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and PD0325901 | | 分子名称: | CHLORIDE ION, Dual specificity mitogen-activated protein kinase kinase 1, GLYCEROL, ... | | 著者 | Li, K, Gonzalez Del-Pino, G, Ha, B.H, Park, E, Eck, M.J. | | 登録日 | 2021-03-11 | | 公開日 | 2021-04-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.47 Å) | | 主引用文献 | Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7M0W
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Pimasertib | | 分子名称: | Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, N-[(2S)-2,3-dihydroxypropyl]-3-[(2-fluoro-4-iodophenyl)amino]pyridine-4-carboxamide, ... | | 著者 | Li, K, Gonzalez Del-Pino, G, Ha, B.H, Park, E, Eck, M.J. | | 登録日 | 2021-03-11 | | 公開日 | 2021-04-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.09 Å) | | 主引用文献 | Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7M0V
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Cobimetinib | | 分子名称: | Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | 著者 | Li, K, Gonzalez Del-Pino, G, Ha, B.H, Park, E, Eck, M.J. | | 登録日 | 2021-03-11 | | 公開日 | 2021-04-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.16 Å) | | 主引用文献 | Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7M0U
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Binimetinib | | 分子名称: | 5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide, Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, ... | | 著者 | Li, K, Gonzalez Del-Pino, G, Ha, B.H, Park, E, Eck, M.J. | | 登録日 | 2021-03-11 | | 公開日 | 2021-04-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.09 Å) | | 主引用文献 | Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7M0T
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Selumetinib | | 分子名称: | 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide, Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, ... | | 著者 | Li, K, Gonzalez Del-Pino, G, Ha, B.H, Park, E, Eck, M.J. | | 登録日 | 2021-03-11 | | 公開日 | 2021-04-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.19 Å) | | 主引用文献 | Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7JV1
 | | Crystal Structure of KSR1:MEK1 in complex with AMP-PNP, and allosteric MEK inhibitor APS-9-95-1 | | 分子名称: | Dual specificity mitogen-activated protein kinase kinase 1, Kinase suppressor of Ras 1, MAGNESIUM ION, ... | | 著者 | Khan, Z.M, Dar, A.C, Scopton, A.P. | | 登録日 | 2020-08-20 | | 公開日 | 2020-09-30 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.62 Å) | | 主引用文献 | Structural basis for the action of the drug trametinib at KSR-bound MEK.
Nature, 588, 2020
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7JV0
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7JUZ
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7JUY
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7JUX
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7JUW
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7JUV
 | | Crystal Structure of KSR2:MEK1 in complex with AMP-PNP, and allosteric MEK inhibitor APS-9-95-1 | | 分子名称: | Dual specificity mitogen-activated protein kinase kinase 1, Kinase suppressor of Ras 2, MAGNESIUM ION, ... | | 著者 | Khan, Z.M, Dar, A.C, Scopton, A.P. | | 登録日 | 2020-08-20 | | 公開日 | 2020-09-30 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.36 Å) | | 主引用文献 | 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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7JUT
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7JUS
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7JUR
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7JUQ
 | | Crystal Structure of KSR2:MEK1 in complex with ADP | | 分子名称: | ADENOSINE-5'-DIPHOSPHATE, Dual specificity mitogen-activated protein kinase kinase 1, Kinase suppressor of Ras 2, ... | | 著者 | Khan, Z.M, Dar, A.C. | | 登録日 | 2020-08-20 | | 公開日 | 2020-09-30 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.22 Å) | | 主引用文献 | Structural basis for the action of the drug trametinib at KSR-bound MEK.
Nature, 588, 2020
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7F2X
 | | Crystal structure of MEK1 C121S mutant | | 分子名称: | MEK1 F11, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER | | 著者 | Fujioka, Y, Noda, N.N. | | 登録日 | 2021-06-15 | | 公開日 | 2022-06-22 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (2.007 Å) | | 主引用文献 | Qualitative differences in disease-associated MEK mutants reveal molecular signatures and aberrant signaling-crosstalk in cancer.
Nat Commun, 13, 2022
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7ENJ
 | | Human Mediator (deletion of MED1-IDR) in a Tail-bent conformation (MED-B) | | 分子名称: | Isoform 2 of Mediator of RNA polymerase II transcription subunit 8, Mediator of RNA polymerase II transcription subunit 1, Mediator of RNA polymerase II transcription subunit 10, ... | | 著者 | Yin, X, Li, J, Wu, Z, Liu, W, Xu, Y. | | 登録日 | 2021-04-17 | | 公開日 | 2021-05-19 | | 最終更新日 | 2021-06-16 | | 実験手法 | ELECTRON MICROSCOPY (4.4 Å) | | 主引用文献 | Structures of the human Mediator and Mediator-bound preinitiation complex.
Science, 372, 2021
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7EMF
 | | Human Mediator (deletion of MED1-IDR) in a Tail-extended conformation | | 分子名称: | Isoform 2 of Mediator of RNA polymerase II transcription subunit 16, Isoform 2 of Mediator of RNA polymerase II transcription subunit 8, Mediator of RNA polymerase II transcription subunit 1, ... | | 著者 | Yin, X, Li, J, Wu, Z, Liu, W, Xu, Y. | | 登録日 | 2021-04-13 | | 公開日 | 2021-05-05 | | 最終更新日 | 2021-06-16 | | 実験手法 | ELECTRON MICROSCOPY (3.5 Å) | | 主引用文献 | Structures of the human Mediator and Mediator-bound preinitiation complex.
Science, 372, 2021
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7E75
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7E73
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7AUV
 | | The structure of ERK2 in complex with dual inhibitor ASTX029 | | 分子名称: | (2~{R})-2-[5-[5-chloranyl-2-(oxan-4-ylamino)pyrimidin-4-yl]-3-oxidanylidene-1~{H}-isoindol-2-yl]-~{N}-[(1~{S})-1-(3-fluoranyl-5-methoxy-phenyl)-2-oxidanyl-ethyl]propanamide, DIMETHYL SULFOXIDE, Mitogen-activated protein kinase 1, ... | | 著者 | O'Reilly, M. | | 登録日 | 2020-11-03 | | 公開日 | 2021-10-06 | | 最終更新日 | 2021-10-13 | | 実験手法 | X-RAY DIFFRACTION (1.76 Å) | | 主引用文献 | ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK.
Mol.Cancer Ther., 20, 2021
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