7F2X
 
 | | Crystal structure of MEK1 C121S mutant | | Descriptor: | MEK1 F11, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER | | Authors: | Fujioka, Y, Noda, N.N. | | Deposit date: | 2021-06-15 | | Release date: | 2022-06-22 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.007 Å) | | Cite: | Qualitative differences in disease-associated MEK mutants reveal molecular signatures and aberrant signaling-crosstalk in cancer.
Nat Commun, 13, 2022
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8CHF
 | | cryo-EM Structure of Craf:14-3-3:Mek1 | | Descriptor: | 14-3-3 protein zeta isoform X1, 2-{4-[(1E)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3-(pyridin-4-yl)-1H-pyrazol-1-yl}ethanol, Dual specificity mitogen-activated protein kinase kinase 1, ... | | Authors: | Dedden, D, Ulrich, G. | | Deposit date: | 2023-02-07 | | Release date: | 2024-02-21 | | Last modified: | 2024-02-28 | | Method: | ELECTRON MICROSCOPY (4.25 Å) | | Cite: | Cryo-EM Structures of CRAF 2 /14-3-3 2 and CRAF 2 /14-3-3 2 /MEK1 2 Complexes.
J.Mol.Biol., 436, 2024
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7PQV
 | | MEK1 IN COMPLEX WITH COMPOUND 7 | | Descriptor: | 8-(2-chloranyl-4-methoxy-phenyl)-7-fluoranyl-1-piperidin-4-yl-imidazo[4,5-c]quinoline, CALCIUM ION, Dual specificity mitogen-activated protein kinase kinase 1, ... | | Authors: | Moebitz, H. | | Deposit date: | 2021-09-20 | | Release date: | 2022-03-16 | | Last modified: | 2024-06-19 | | Method: | X-RAY DIFFRACTION (2.13 Å) | | Cite: | Discovery of MAP855, an Efficacious and Selective MEK1/2 Inhibitor with an ATP-Competitive Mode of Action.
J.Med.Chem., 65, 2022
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4MNE
 | | Crystal structure of the BRAF:MEK1 complex | | Descriptor: | 7-fluoro-3-[(2-fluoro-4-iodophenyl)amino]-N-{[(2S)-2-hydroxypropyl]oxy}furo[3,2-c]pyridine-2-carboxamide, CHLORIDE ION, Dual specificity mitogen-activated protein kinase kinase 1, ... | | Authors: | Sudhamsu, J, Haling, J.R, Morales, T, Brandhuber, B, Hymowitz, S.G. | | Deposit date: | 2013-09-10 | | Release date: | 2014-06-18 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.8483 Å) | | Cite: | Structure of the BRAF-MEK Complex Reveals a Kinase Activity Independent Role for BRAF in MAPK Signaling.
Cancer Cell, 26, 2014
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5YT3
 | | Structure of the Human Mitogen-Activated Protein Kinase Kinase 1 S218D and S222D mutant | | Descriptor: | MAGNESIUM ION, Mitogen-activated protein kinase kinase 1, isoform CRA_d, ... | | Authors: | Nakae, S, Doko, K, Tada, T, Shirai, T. | | Deposit date: | 2017-11-16 | | Release date: | 2018-11-21 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Structure of the Human Mitogen-Activated Protein Kinase Kinase 1 S218D and S222D mutant
To Be Published
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5HZE
 | | Mek1 adopts DFG-out conformation when bound to an analog of E6201. | | Descriptor: | (3S,4R,8S,9S,11E)-8,9,16-trihydroxy-3,4-dimethyl-14-(methylamino)-3,4,5,6,9,10-hexahydro-1H-2-benzoxacyclotetradecine-1,7(8H)-dione, Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION | | Authors: | Larsen, N.A, Bloudoff, K. | | Deposit date: | 2016-02-02 | | Release date: | 2017-05-03 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Mek1 adopts DFG-out conformation when bound to an analog of E6201.
To Be Published
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3MBL
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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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2P55
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5EYM
 | | MEK1 IN COMPLEX WITH BI 847325 | | Descriptor: | 3-[(3~{Z})-3-[[[4-[(dimethylamino)methyl]phenyl]amino]-phenyl-methylidene]-2-oxidanylidene-1~{H}-indol-6-yl]-~{N}-ethyl-prop-2-ynamide, CALCIUM ION, Dual specificity mitogen-activated protein kinase kinase 1 | | Authors: | Bader, G, Reiser, U, Zahn, S.K, Treu, M. | | Deposit date: | 2015-11-25 | | Release date: | 2016-08-17 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases.
Mol.Cancer Ther., 15, 2016
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5BX0
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4LMN
 | | Crystal Structure of MEK1 kinase bound to GDC0973 | | Descriptor: | Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | Authors: | Ultsch, M.H. | | Deposit date: | 2013-07-10 | | Release date: | 2013-08-07 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers.
Nature, 501, 2013
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1S9J
 | | X-ray structure of the human mitogen-activated protein kinase kinase 1 (MEK1) in a complex with ligand and MgATP | | Descriptor: | 5-BROMO-N-(2,3-DIHYDROXYPROPOXY)-3,4-DIFLUORO-2-[(2-FLUORO-4-IODOPHENYL)AMINO]BENZAMIDE, ADENOSINE-5'-TRIPHOSPHATE, Dual specificity mitogen-activated protein kinase kinase 1, ... | | Authors: | Ohren, J.F, Chen, H, Pavlovsky, A, Whitehead, C, Yan, C, McConnell, P, Delaney, A, Dudley, D.T, Sebolt-Leopold, J, Hasemann, C.A. | | Deposit date: | 2004-02-04 | | Release date: | 2004-11-23 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition.
Nat.Struct.Mol.Biol., 11, 2004
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7B7R
 | | MEK1 in complex with compound 4 | | Descriptor: | 2-[5-[ethyl(methyl)amino]imidazo[1,2-a]pyrimidin-7-yl]phenol, Dual specificity mitogen-activated protein kinase kinase 1,Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, ... | | Authors: | Kack, H, Oster, L. | | Deposit date: | 2020-12-11 | | Release date: | 2021-03-03 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Fragment-Based Discovery of Novel Allosteric MEK1 Binders.
Acs Med.Chem.Lett., 12, 2021
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7B3M
 | | MEK1 in complex with compound 6 | | Descriptor: | 1~{H}-indol-2-yl(pyridin-3-yl)methanone, Dual specificity mitogen-activated protein kinase kinase 1,Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, ... | | Authors: | Kack, H, Oster, L. | | Deposit date: | 2020-12-01 | | Release date: | 2021-03-03 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Fragment-Based Discovery of Novel Allosteric MEK1 Binders.
Acs Med.Chem.Lett., 12, 2021
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6U2G
 | | BRAF-MEK complex with AMP-PCP bound to BRAF | | Descriptor: | Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER, ... | | Authors: | Liau, N.P.D, Wendorff, T, Hymowitz, S, Sudhamsu, J. | | Deposit date: | 2019-08-19 | | Release date: | 2019-08-28 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.886 Å) | | Cite: | Negative regulation of RAF kinase activity by ATP is overcome by 14-3-3-induced dimerization.
Nat.Struct.Mol.Biol., 27, 2020
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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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6V2W
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP | | Descriptor: | Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | Authors: | Li, K, Gonzalez Del-Pino, G, Park, E, Eck, M.J. | | Deposit date: | 2019-11-25 | | Release date: | 2020-12-02 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3.12 Å) | | Cite: | Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7B9L
 | | MEK1 in complex with compound 23 | | Descriptor: | Dual specificity mitogen-activated protein kinase kinase 1,Dual specificity mitogen-activated protein kinase kinase 1, GLYCEROL, MAGNESIUM ION, ... | | Authors: | Kack, H, Oster, L. | | Deposit date: | 2020-12-14 | | Release date: | 2021-03-03 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Fragment-Based Discovery of Novel Allosteric MEK1 Binders.
Acs Med.Chem.Lett., 12, 2021
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7B94
 | | MEK1 in complex with compound 6 | | Descriptor: | 2-(4-iodophenyl)-8~{H}-imidazo[1,2-c]pyrimidin-5-one, Dual specificity mitogen-activated protein kinase kinase 1,Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, ... | | Authors: | Kack, H, Oster, L. | | Deposit date: | 2020-12-14 | | Release date: | 2021-03-03 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Fragment-Based Discovery of Novel Allosteric MEK1 Binders.
Acs Med.Chem.Lett., 12, 2021
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6PP9
 | | Crystal structure of BRAF:MEK1 complex | | Descriptor: | 5-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)imidazo[1,5-a]pyridine-6-carboxamide, CHLORIDE ION, Dual specificity mitogen-activated protein kinase kinase 1, ... | | Authors: | Li, K, Gonzalez Del-Pino, G, Park, E, Eck, M.J. | | Deposit date: | 2019-07-05 | | Release date: | 2019-10-09 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.59 Å) | | Cite: | Architecture of autoinhibited and active BRAF-MEK1-14-3-3 complexes.
Nature, 575, 2019
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6Q0J
 | | 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, Dual specificity mitogen-activated protein kinase kinase 1, ... | | Authors: | Park, E, Rawson, S, Jeon, H, Eck, M.J. | | Deposit date: | 2019-08-01 | | Release date: | 2019-10-09 | | Last modified: | 2020-04-22 | | Method: | ELECTRON MICROSCOPY (4.9 Å) | | Cite: | Architecture of autoinhibited and active BRAF-MEK1-14-3-3 complexes.
Nature, 575, 2019
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6X2S
 | | Crystal Structure of Mek1(NQ)NES peptide bound to CRM | | Descriptor: | Dual specificity mitogen-activated protein kinase kinase 1, Exportin-1, GLYCEROL, ... | | Authors: | Baumhardt, J.M. | | Deposit date: | 2020-05-20 | | Release date: | 2020-07-01 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.496 Å) | | Cite: | Recognition of nuclear export signals by CRM1 carrying the oncogenic E571K mutation.
Mol.Biol.Cell, 31, 2020
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6X2P
 | | Crystal Structure of the Mek1NES peptide bound to CRM1 | | Descriptor: | Dual specificity mitogen-activated protein kinase kinase 1, Exportin-1, GLYCEROL, ... | | Authors: | Baumhardt, J.M. | | Deposit date: | 2020-05-20 | | Release date: | 2020-07-01 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.401 Å) | | Cite: | Recognition of nuclear export signals by CRM1 carrying the oncogenic E571K mutation.
Mol.Biol.Cell, 31, 2020
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