6UUO
 
 | | Crystal structure of BRAF kinase domain bound to the PROTAC P4B | | Descriptor: | N-(3-{5-[(1-acetylpiperidin-4-yl)(methyl)amino]-3-(pyrimidin-5-yl)-1H-pyrrolo[3,2-b]pyridin-1-yl}-2,4-difluorophenyl)propane-1-sulfonamide, Serine/threonine-protein kinase B-raf | | Authors: | Maisonneuve, P, Posternak, G, Kurinov, I, Sicheri, F. | | Deposit date: | 2019-10-30 | | Release date: | 2020-06-03 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3.288 Å) | | Cite: | Functional characterization of a PROTAC directed against BRAF mutant V600E.
Nat.Chem.Biol., 16, 2020
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6CAD
 | | Crystal structure of RAF kinase domain bound to the inhibitor 2a | | Descriptor: | 1-(propan-2-yl)-3-({3-[3-(trifluoromethyl)phenyl]isoquinolin-8-yl}ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Serine/threonine-protein kinase B-raf | | Authors: | Maisonneuve, P, Kurinov, I, Assadieskandar, A, Yu, C, Liu, X, Chen, Y.-C, Prakash, G.K.S, Zhang, C, SIcheri, F. | | Deposit date: | 2018-01-30 | | Release date: | 2018-02-21 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.55 Å) | | Cite: | Effects of rigidity on the selectivity of protein kinase inhibitors.
Eur J Med Chem, 146, 2018
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8BW8
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8BW9
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6NTD
 | | Crystal Structure of G12V HRas-GppNHp bound in complex with the engineered RBD variant 12 of CRAF Kinase protein | | Descriptor: | GTPase HRas, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER, ... | | Authors: | Maisonneuve, P, Kurinov, I, Wiechmann, S, Ernst, A, Sicheri, F. | | Deposit date: | 2019-01-28 | | Release date: | 2020-03-04 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3.15 Å) | | Cite: | Conformation-specific inhibitors of activated Ras GTPases reveal limited Ras dependency of patient-derived cancer organoids.
J.Biol.Chem., 295, 2020
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6NTC
 | | Crystal Structure of G12V HRas-GppNHp bound in complex with the engineered RBD variant 1 of CRAF Kinase protein | | Descriptor: | GLYCEROL, GTPase HRas, MAGNESIUM ION, ... | | Authors: | Maisonneuve, P, Kurinov, I, Wiechmann, S, Ernst, A, Sicheri, F. | | Deposit date: | 2019-01-28 | | Release date: | 2020-03-04 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Conformation-specific inhibitors of activated Ras GTPases reveal limited Ras dependency of patient-derived cancer organoids.
J.Biol.Chem., 295, 2020
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6NSQ
 | | Crystal structure of BRAF kinase domain bound to the inhibitor 2l | | Descriptor: | 5-[(4-amino-1-ethyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)ethynyl]-N-(4-chlorophenyl)-6-methylisoquinolin-1-amine, Serine/threonine-protein kinase B-raf | | Authors: | Maisonneuve, P, Kurinov, I, Assadieskandar, A, Yu, C, Zhang, C, Sicheri, F. | | Deposit date: | 2019-01-25 | | Release date: | 2019-06-19 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3.05 Å) | | Cite: | Rigidification Dramatically Improves Inhibitor Selectivity for RAF Kinases.
Acs Med.Chem.Lett., 10, 2019
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5EYZ
 | | CRYSTAL STRUCTURE OF THE PTPN4 PDZ DOMAIN COMPLEXED WITH THE TAILORED PEPTIDE CYTO8-RETEV | | Descriptor: | CHLORIDE ION, CYTO8-RETEV, Tyrosine-protein phosphatase non-receptor type 4 | | Authors: | Maisonneuve, P, Vaney, M.C, Babault, B, Caillet-Saguy, C, Lafon, M, Delepierre, M, Cordier, F, Wolff, N. | | Deposit date: | 2015-11-26 | | Release date: | 2016-06-08 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.09 Å) | | Cite: | Molecular Basis of the Interaction of the Human Protein Tyrosine Phosphatase Non-receptor Type 4 (PTPN4) with the Mitogen-activated Protein Kinase p38 gamma.
J.Biol.Chem., 291, 2016
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5EZ0
 | | CRYSTAL STRUCTURE OF THE PTPN4 PDZ DOMAIN COMPLEXED WITH THE PDZ BINDING MOTIF OF THE MITOGEN ACTIVATED PROTEIN KINASE P38GAMMA. | | Descriptor: | Mitogen-activated protein kinase 12, SULFATE ION, Tyrosine-protein phosphatase non-receptor type 4 | | Authors: | Maisonneuve, P, Vaney, M.C, Caillet-Saguy, C, Lafon, M, Delepierre, M, Cordier, F, Wolff, N. | | Deposit date: | 2015-11-26 | | Release date: | 2016-06-08 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.35 Å) | | Cite: | Molecular Basis of the Interaction of the Human Protein Tyrosine Phosphatase Non-receptor Type 4 (PTPN4) with the Mitogen-activated Protein Kinase p38 gamma.
J.Biol.Chem., 291, 2016
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5VYK
 | | Crystal structure of the BRS domain of BRAF in complex with the CC-SAM domain of KSR1 | | Descriptor: | Chimera protein of BRS domain of BRAF and CC-SAM domain of KSR1,Serine/threonine-protein kinase B-raf, GLYCEROL | | Authors: | Maisonneuve, P, Kurinov, I, Marullo, S.A, Lavoie, H, Thevakumaran, N, Sahmi, M, Jin, T, Therrien, M, SIcheri, F. | | Deposit date: | 2017-05-25 | | Release date: | 2018-02-14 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (1.749 Å) | | Cite: | MEK drives BRAF activation through allosteric control of KSR proteins.
Nature, 554, 2018
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5VR3
 | | Crystal structure of the BRS domain of BRAF | | Descriptor: | BRAF, SULFATE ION | | Authors: | Thevakumaran, N, Maisonneuve, P, Kurinov, I, Lavoie, H, Marullo, S.A, Sahmi, M, Jin, T, Therrien, M, Sicheri, F. | | Deposit date: | 2017-05-10 | | Release date: | 2018-02-14 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.102 Å) | | Cite: | MEK drives BRAF activation through allosteric control of KSR proteins.
Nature, 554, 2018
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