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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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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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
 | | 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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1LUZ
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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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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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4LGH
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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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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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7JUX
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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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7JUT
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7JUS
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7JV0
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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
 | | 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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7JUZ
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7JUU
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7JUY
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