7E2K
 
 | | Crystal structure of the RWD domain of human GCN2 - 1 | | Descriptor: | eIF-2-alpha kinase GCN2 | | Authors: | Hei, Z, Zhou, J, Liu, Z, Wang, J, Fang, P. | | Deposit date: | 2021-02-05 | | Release date: | 2021-03-17 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.041 Å) | | Cite: | Crystal structures reveal a novel dimer of the RWD domain of human general control nonderepressible 2.
Biochem.Biophys.Res.Commun., 549, 2021
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7QWK
 | | GCN2 (EIF2ALPHA KINASE 4, E2AK4) IN COMPLEX WITH COMPOUND 2 | | Descriptor: | (2~{S})-~{N}-[(1~{S})-1-[4-[(6-pyridin-4-ylquinazolin-2-yl)amino]phenyl]ethyl]piperidine-2-carboxamide, DIMETHYL SULFOXIDE, eIF-2-alpha kinase GCN2 | | Authors: | Maia de Oliveira, T. | | Deposit date: | 2022-01-25 | | Release date: | 2022-05-04 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | The structure of human GCN2 reveals a parallel, back-to-back kinase dimer with a plastic DFG activation loop motif.
Biochem.J., 477, 2020
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7E2M
 | | Crystal structure of the RWD domain of human GCN2 - 2 | | Descriptor: | eIF-2-alpha kinase GCN2 | | Authors: | Hei, Z, Zhou, J, Liu, Z, Wang, J, Fang, P. | | Deposit date: | 2021-02-05 | | Release date: | 2021-03-17 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.35 Å) | | Cite: | Crystal structures reveal a novel dimer of the RWD domain of human general control nonderepressible 2.
Biochem.Biophys.Res.Commun., 549, 2021
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6N3O
 | | Identification of novel, potent and selective GCN2 inhibitors as first-in-class anti-tumor agents | | Descriptor: | N-{3-[(2-aminopyrimidin-5-yl)ethynyl]-2,4-difluorophenyl}-5-chloro-2-methoxypyridine-3-sulfonamide, eIF-2-alpha kinase GCN2 | | Authors: | Hoffman, I.D, Fujimoto, J, Kurasawa, O, Takagi, T, Klein, M.G, Kefala, G, Ding, S.C, Cary, D.R, Mizojiri, R. | | Deposit date: | 2018-11-15 | | Release date: | 2019-10-09 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode.
Acs Med.Chem.Lett., 10, 2019
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6N3L
 | | Identification of novel, potent and selective GCN2 inhibitors as first-in-class anti-tumor agents | | Descriptor: | N-{6-[(1-methyl-2-{[4-(trifluoromethyl)phenyl]amino}-1H-benzimidazol-5-yl)oxy]pyrimidin-4-yl}cyclopropanecarboxamide, eIF-2-alpha kinase GCN2,eIF-2-alpha kinase GCN2 | | Authors: | Hoffman, I.D, Fujimoto, J, Kurasawa, O, Takagi, T, Klein, M.G, Kefala, G, Ding, S.C, Cary, D.R, Mizojiri, R. | | Deposit date: | 2018-11-15 | | Release date: | 2019-10-09 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.61 Å) | | Cite: | Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode.
Acs Med.Chem.Lett., 10, 2019
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7QQ6
 | | GCN2 (EIF2ALPHA KINASE 4, E2AK4) IN COMPLEX WITH COMPOUND 1 (dovitinib) | | Descriptor: | 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one, eIF-2-alpha kinase GCN2 | | Authors: | Maia de Oliveira, T. | | Deposit date: | 2022-01-06 | | Release date: | 2022-03-02 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | The structure of human GCN2 reveals a parallel, back-to-back kinase dimer with a plastic DFG activation loop motif.
Biochem.J., 477, 2020
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6N3N
 | | Identification of novel, potent and selective GCN2 inhibitors as first-in-class anti-tumor agents | | Descriptor: | N-{3-[(2-aminopyrimidin-5-yl)ethynyl]-2,4-difluorophenyl}-2,5-dichloro-3-(hydroxymethyl)benzene-1-sulfonamide, eIF-2-alpha kinase GCN2,eIF-2-alpha kinase GCN2 | | Authors: | Hoffman, I.D, Fujimoto, J, Kurasawa, O, Takagi, T, Klein, M.G, Kefala, G, Ding, S.C, Cary, D.R, Mizojiri, R. | | Deposit date: | 2018-11-15 | | Release date: | 2019-10-09 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (3.01 Å) | | Cite: | Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode.
Acs Med.Chem.Lett., 10, 2019
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8T7T
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