5TPQ
 
 | | E. coli alkaline phosphatase D101A, D153A, R166S, E322A, K328A mutant | | Descriptor: | Alkaline phosphatase, PHOSPHATE ION, ZINC ION | | Authors: | Sunden, F, AlSadhan, I, Lyubimov, A.Y, Doukov, T, Swan, J, Herschlag, D. | | Deposit date: | 2016-10-20 | | Release date: | 2017-11-01 | | Last modified: | 2024-10-30 | | Method: | X-RAY DIFFRACTION (2.45 Å) | | Cite: | Differential catalytic promiscuity of the alkaline phosphatase superfamily bimetallo core reveals mechanistic features underlying enzyme evolution.
J. Biol. Chem., 292, 2017
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5TOO
 | | Crystal structure of alkaline phosphatase PafA T79S, N100A, K162A, R164A mutant | | Descriptor: | Alkaline phosphatase PafA, CHLORIDE ION, ZINC ION | | Authors: | Lyubimov, A.Y, Sunden, F, AlSadhan, I, Herschlag, D. | | Deposit date: | 2016-10-18 | | Release date: | 2017-11-01 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.031 Å) | | Cite: | Differential catalytic promiscuity of the alkaline phosphatase superfamily bimetallo core reveals mechanistic features underlying enzyme evolution.
J. Biol. Chem., 292, 2017
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5QTZ
 | | TGF-BETA RECEPTOR TYPE 1 KINASE DOMAIN (T204D) IN COMPLEX WITH 6-[1-(2,2-DIFLUOROETHYL)-4-(6-METHYLPYRIDIN-2-YL)-1H-IMIDAZOL-5-YL]IMIDAZO[1,2-A]PYRIDINE | | Descriptor: | 6-[1-(2,2-difluoroethyl)-4-(6-methylpyridin-2-yl)-1H-imidazol-5-yl]imidazo[1,2-a]pyridine, GLYCEROL, TGF-beta receptor type-1 | | Authors: | Sheriff, S. | | Deposit date: | 2019-11-19 | | Release date: | 2020-02-05 | | Last modified: | 2024-05-22 | | Method: | X-RAY DIFFRACTION (1.83 Å) | | Cite: | Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGF beta R1 Inhibitor as an Immuno-oncology Agent.
Acs Med.Chem.Lett., 11, 2020
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5QU0
 | | TGF-BETA RECEPTOR TYPE 1 KINASE DOMAIN (T204D) IN COMPLEX WITH 6-[4-(3-CHLORO-4-FLUOROPHENYL)-1-(2-HYDROXYETHYL)-1H-IMIDAZOL-5-YL]IMIDAZO[1,2-B]PYRIDAZINE-3-CARBONITRILE | | Descriptor: | 6-[4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidazol-5-yl]imidazo[1,2-b]pyridazine-3-carbonitrile, GLYCEROL, TGF-beta receptor type-1 | | Authors: | Sheriff, S. | | Deposit date: | 2019-11-19 | | Release date: | 2020-02-05 | | Last modified: | 2024-05-22 | | Method: | X-RAY DIFFRACTION (1.67 Å) | | Cite: | Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGF beta R1 Inhibitor as an Immuno-oncology Agent.
Acs Med.Chem.Lett., 11, 2020
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5QIN
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5QIM
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5QIK
 | | TGF-BETA RECEPTOR TYPE 1 KINASE DOMAIN (T204D) IN COMPLEX WITH N-{4-[3-(6-fluoropyridin-3-yl)-4-oxo-4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-2-yl]pyridin-2-yl}acetamide | | Descriptor: | GLYCEROL, N-{4-[3-(6-fluoropyridin-3-yl)-4-oxo-4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-2-yl]pyridin-2-yl}acetamide, TGF-beta receptor type-1 | | Authors: | Sheriff, S. | | Deposit date: | 2018-08-05 | | Release date: | 2018-10-31 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (1.58 Å) | | Cite: | Discovery of 4-Azaindole Inhibitors of TGF beta RI as Immuno-oncology Agents.
ACS Med Chem Lett, 9, 2018
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5QIL
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6PDJ
 | | Tyrosine-protein kinase LCK bound to Compound 11 | | Descriptor: | 3-CYCLOHEXYL-1-PROPYLSULFONIC ACID, N-{4-[(6-methoxypyrazolo[1,5-a]pyridine-3-carbonyl)amino]-3-methylphenyl}-1-methyl-1H-indazole-3-carboxamide, NICKEL (II) ION, ... | | Authors: | Critton, D.A. | | Deposit date: | 2019-06-19 | | Release date: | 2019-10-09 | | Last modified: | 2024-10-30 | | Method: | X-RAY DIFFRACTION (1.81 Å) | | Cite: | Discovery of Pyridazinone and Pyrazolo[1,5-a]pyridine Inhibitors of C-Terminal Src Kinase.
Acs Med.Chem.Lett., 10, 2019
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7T1Y
 | | Structure of the Fbw7-Skp1-MycCdegron complex | | Descriptor: | F-box/WD repeat-containing protein 7, Myc proto-oncogene protein C terminal degron, S-phase kinase-associated protein 1, ... | | Authors: | Wang, B, Rusnac, D.V, Clurman, B.E, Zheng, N. | | Deposit date: | 2021-12-02 | | Release date: | 2022-02-16 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.55 Å) | | Cite: | Two diphosphorylated degrons control c-Myc degradation by the Fbw7 tumor suppressor.
Sci Adv, 8, 2022
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7T1Z
 | | Structure of the Fbw7-Skp1-MycNdegron complex | | Descriptor: | F-box/WD repeat-containing protein 7, Myc proto-oncogene N terminal degron, S-phase kinase-associated protein 1, ... | | Authors: | Wang, B, Rusnac, D.V, Clurman, B.E, Zheng, N. | | Deposit date: | 2021-12-02 | | Release date: | 2022-02-16 | | Last modified: | 2024-10-23 | | Method: | X-RAY DIFFRACTION (2.77 Å) | | Cite: | Two diphosphorylated degrons control c-Myc degradation by the Fbw7 tumor suppressor.
Sci Adv, 8, 2022
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