7M0V
 
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Cobimetinib | | Descriptor: | Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | Authors: | Li, K, Gonzalez Del-Pino, G, Ha, B.H, Park, E, Eck, M.J. | | Deposit date: | 2021-03-11 | | Release date: | 2021-04-21 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (3.16 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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7M0W
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Pimasertib | | Descriptor: | Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, N-[(2S)-2,3-dihydroxypropyl]-3-[(2-fluoro-4-iodophenyl)amino]pyridine-4-carboxamide, ... | | Authors: | Li, K, Gonzalez Del-Pino, G, Ha, B.H, Park, E, Eck, M.J. | | Deposit date: | 2021-03-11 | | Release date: | 2021-04-21 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (3.09 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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7M0U
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Binimetinib | | Descriptor: | 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, ... | | Authors: | Li, K, Gonzalez Del-Pino, G, Ha, B.H, Park, E, Eck, M.J. | | Deposit date: | 2021-03-11 | | Release date: | 2021-04-21 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (3.09 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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7M0Y
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Trametinib | | Descriptor: | Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | Authors: | Li, K, Gonzalez Del-Pino, G, Ha, B.H, Park, E, Eck, M.J. | | Deposit date: | 2021-03-11 | | Release date: | 2021-04-21 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (3.45 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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7M0T
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Selumetinib | | Descriptor: | 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, ... | | Authors: | Li, K, Gonzalez Del-Pino, G, Ha, B.H, Park, E, Eck, M.J. | | Deposit date: | 2021-03-11 | | Release date: | 2021-04-21 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (3.19 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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7LTX
 | | EGFR (T790M/V948R) in complex with quinazolinone allosteric inhibitor | | Descriptor: | (2R)-2-{5-fluoro-6-[4-(1-methylpiperidin-4-yl)phenyl]-4-oxoquinazolin-3(4H)-yl}-2-phenyl-N-(1,3-thiazol-2-yl)acetamide, Epidermal growth factor receptor, MAGNESIUM ION, ... | | Authors: | Beyett, T.S, Eck, M.J. | | Deposit date: | 2021-02-20 | | Release date: | 2022-02-23 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC.
Bioorg.Med.Chem.Lett., 68, 2022
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7LG8
 | | EGFR (T79M/V948R) in complex with naquotinib and an allosteric inhibitor | | Descriptor: | (2R)-2-(5-fluoro-2-hydroxyphenyl)-2-{6-[4-(1-methylpiperidin-4-yl)phenyl]-1-oxo-1,3-dihydro-2H-isoindol-2-yl}-N-(1,3-thiazol-2-yl)acetamide, 6-ethyl-3-[[4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]amino]-5-[(3R)-1-prop-2-enoylpyrrolidin-3-yl]oxy-pyrazin e-2-carboxamide, Epidermal growth factor receptor | | Authors: | Beyett, T.S, Eck, M.J. | | Deposit date: | 2021-01-19 | | Release date: | 2022-02-23 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.93 Å) | | Cite: | Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors.
Nat Commun, 13, 2022
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7UKV
 | | Wild type EGFR in complex with Lazertinib (YH25448) | | Descriptor: | Epidermal growth factor receptor, N-[5-{[(4P)-4-{4-[(dimethylamino)methyl]-3-phenyl-1H-pyrazol-1-yl}pyrimidin-2-yl]amino}-4-methoxy-2-(morpholin-4-yl)phenyl]propanamide | | Authors: | Beyett, T.S, Pham, C, Eck, M.J, Heppner, D.E. | | Deposit date: | 2022-04-02 | | Release date: | 2022-11-23 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448).
Acs Med.Chem.Lett., 13, 2022
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7MYX
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3O0Z
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3OKQ
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3ONX
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6P1L
 | | Crystal structure of EGFR in complex with EAI045 | | Descriptor: | (2R)-2-(5-fluoro-2-hydroxyphenyl)-2-(1-oxo-1,3-dihydro-2H-isoindol-2-yl)-N-(1,3-thiazol-2-yl)acetamide, Epidermal growth factor receptor, MAGNESIUM ION, ... | | Authors: | Heppner, D.E, Eck, M.J. | | Deposit date: | 2019-05-20 | | Release date: | 2019-12-18 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors.
Acs Med.Chem.Lett., 10, 2019
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6P1D
 | | Crystal structure of EGFR with mutant-selective dihydrodibenzodiazepinone allosteric inhibitor | | Descriptor: | 10-benzyl-8-fluoro-5,10-dihydro-11H-dibenzo[b,e][1,4]diazepin-11-one, Epidermal growth factor receptor, MAGNESIUM ION, ... | | Authors: | Heppner, D.E, Eck, M.J. | | Deposit date: | 2019-05-19 | | Release date: | 2019-12-18 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors.
Acs Med.Chem.Lett., 10, 2019
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6P8Q
 | | EGFR in complex with a dihydrodibenzodiazepinone allosteric inhibitor. | | Descriptor: | 1,2-ETHANEDIOL, 10-benzyl-2-fluoro-5,10-dihydro-11H-dibenzo[b,e][1,4]diazepin-11-one, ADENOSINE MONOPHOSPHATE, ... | | Authors: | Yun, C.H, Heppner, D.E, Eck, M.J. | | Deposit date: | 2019-06-07 | | Release date: | 2019-12-18 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors.
Acs Med.Chem.Lett., 10, 2019
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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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6Q0K
 | | Structure of a MAPK pathway complex | | Descriptor: | 14-3-3 protein zeta/delta, Serine/threonine-protein kinase B-raf | | 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 (6.8 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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1D4W
 | | CRYSTAL STRUCTURE OF THE XLP PROTEIN SAP IN COMPLEX WITH SLAM PHOSPHOPEPTIDE | | Descriptor: | SIGNALING LYMPHOCYTIC ACTIVATION MOLECULE, T CELL SIGNAL TRANSDUCTION MOLECULE SAP | | Authors: | Poy, F, Yaffe, M.B, Sayos, J, Saxena, K, Eck, M.J. | | Deposit date: | 1999-10-06 | | Release date: | 1999-10-14 | | Last modified: | 2018-01-31 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Crystal structures of the XLP protein SAP reveal a class of SH2 domains with extended, phosphotyrosine-independent sequence recognition.
Mol.Cell, 4, 1999
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1B47
 | | STRUCTURE OF THE N-TERMINAL DOMAIN OF CBL IN COMPLEX WITH ITS BINDING SITE IN ZAP-70 | | Descriptor: | CALCIUM ION, CBL | | Authors: | Meng, W, Sawasdikosol, S, Burakoff, S.J, Eck, M.J. | | Deposit date: | 1999-01-06 | | Release date: | 1999-04-27 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Structure of the amino-terminal domain of Cbl complexed to its binding site on ZAP-70 kinase.
Nature, 398, 1999
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1D1Z
 | | CRYSTAL STRUCTURE OF THE XLP PROTEIN SAP | | Descriptor: | SAP SH2 DOMAIN, SULFATE ION | | Authors: | Poy, F, Yaffe, M.B, Sayos, J, Saxena, K, Eck, M.J. | | Deposit date: | 1999-09-22 | | Release date: | 1999-10-13 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (1.4 Å) | | Cite: | Crystal structures of the XLP protein SAP reveal a class of SH2 domains with extended, phosphotyrosine-independent sequence recognition.
Mol.Cell, 4, 1999
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6Q0T
 | | 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: | 2019-08-02 | | Release date: | 2019-10-09 | | Last modified: | 2020-04-22 | | Method: | ELECTRON MICROSCOPY (5.7 Å) | | Cite: | Architecture of autoinhibited and active BRAF-MEK1-14-3-3 complexes.
Nature, 575, 2019
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1EG3
 | | STRUCTURE OF A DYSTROPHIN WW DOMAIN FRAGMENT IN COMPLEX WITH A BETA-DYSTROGLYCAN PEPTIDE | | Descriptor: | DYSTROPHIN | | Authors: | Huang, X, Poy, F, Zhang, R, Joachimiak, A, Sudol, M, Eck, M.J. | | Deposit date: | 2000-02-11 | | Release date: | 2000-08-23 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Structure of a WW domain containing fragment of dystrophin in complex with beta-dystroglycan.
Nat.Struct.Biol., 7, 2000
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1EG4
 | | STRUCTURE OF A DYSTROPHIN WW DOMAIN FRAGMENT IN COMPLEX WITH A BETA-DYSTROGLYCAN PEPTIDE | | Descriptor: | BETA-DYSTROGLYCAN, DYSTROPHIN | | Authors: | Huang, X, Poy, F, Zhang, R, Joachimiak, A, Sudol, M, Eck, M.J. | | Deposit date: | 2000-02-11 | | Release date: | 2000-08-23 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Structure of a WW domain containing fragment of dystrophin in complex with beta-dystroglycan.
Nat.Struct.Biol., 7, 2000
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1D4T
 | | CRYSTAL STRUCTURE OF THE XLP PROTEIN SAP IN COMPLEX WITH A SLAM PEPTIDE | | Descriptor: | SIGNALING LYMPHOCYTIC ACTIVATION MOLECULE, T CELL SIGNAL TRANSDUCTION MOLECULE SAP | | Authors: | Poy, F, Yaffe, M.B, Sayos, J, Saxena, K, Eck, M.J. | | Deposit date: | 1999-10-06 | | Release date: | 1999-10-14 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (1.1 Å) | | Cite: | Crystal structures of the XLP protein SAP reveal a class of SH2 domains with extended, phosphotyrosine-independent sequence recognition.
Mol.Cell, 4, 1999
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