5NWZ
 
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5NUD
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5LQB
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6YI8
 | | HUMAN FGFR4 KINASE DOMAIN (447-753) IN COMPLEX WITH ROBLITINIB | | Descriptor: | Fibroblast growth factor receptor 4, N-[5-cyano-4-(2-methoxyethylamino)pyridin-2-yl]-7-methanoyl-6-[(4-methyl-2-oxidanylidene-piperazin-1-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide, SULFATE ION | | Authors: | Ostermann, N. | | Deposit date: | 2020-04-01 | | Release date: | 2020-09-30 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (2.13 Å) | | Cite: | Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.
J.Med.Chem., 63, 2020
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6VJT
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6XMX
 | | Cryo-EM structure of BCL6 bound to BI-3802 | | Descriptor: | 2-[6-[[5-chloranyl-2-[(3~{S},5~{R})-3,5-dimethylpiperidin-1-yl]pyrimidin-4-yl]amino]-1-methyl-2-oxidanylidene-quinolin-3-yl]oxy-~{N}-methyl-ethanamide, B-cell lymphoma 6 protein | | Authors: | Yoon, H, Burman, S.S.R, Hunkeler, M, Nowak, R.P, Fischer, E.S. | | Deposit date: | 2020-07-01 | | Release date: | 2020-11-25 | | Last modified: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (3.7 Å) | | Cite: | Small-molecule-induced polymerization triggers degradation of BCL6.
Nature, 588, 2020
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5NH3
 | | CRYSTAL STRUCTURE OF THE Activin receptor type-2A LIGAND BINDING DOMAIN IN COMPLEX WITH BIMAGRUMAB FV | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Activin receptor type-2A, ... | | Authors: | Scheufler, C. | | Deposit date: | 2017-03-21 | | Release date: | 2017-11-15 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.35 Å) | | Cite: | Blockade of activin type II receptors with a dual anti-ActRIIA/IIB antibody is critical to promote maximal skeletal muscle hypertrophy.
Proc. Natl. Acad. Sci. U.S.A., 114, 2017
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5NGV
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5NHW
 | | CRYSTAL STRUCTURE OF THE BIMAGRUMAB Fab | | Descriptor: | GLYCEROL, anti-human ActRII Bimagrumab Fab heavy-chain, anti-human ActRII Bimagrumab Fab light-chain | | Authors: | Rondeau, J.-M. | | Deposit date: | 2017-03-22 | | Release date: | 2017-11-15 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (1.78 Å) | | Cite: | Blockade of activin type II receptors with a dual anti-ActRIIA/IIB antibody is critical to promote maximal skeletal muscle hypertrophy.
Proc. Natl. Acad. Sci. U.S.A., 114, 2017
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5NHR
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8BU9
 | | Structure of DDB1 bound to roscovitine-engaged CDK12-cyclin K | | Descriptor: | Cyclin-K, Cyclin-dependent kinase 12, DNA damage-binding protein 1, ... | | Authors: | Kozicka, Z, Kempf, G, Focht, V, Thoma, N.H. | | Deposit date: | 2022-11-30 | | Release date: | 2023-09-13 | | Last modified: | 2024-03-27 | | Method: | X-RAY DIFFRACTION (3.51 Å) | | Cite: | Design principles for cyclin K molecular glue degraders.
Nat.Chem.Biol., 20, 2024
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8BUS
 | | Structure of DDB1 bound to DS59-engaged CDK12-cyclin K | | Descriptor: | 1,3-dimethyl-5-[[[9-propan-2-yl-6-[(4-pyridin-2-ylphenyl)methylamino]purin-2-yl]amino]methyl]pyrazole-4-sulfonamide, Cyclin-K, Cyclin-dependent kinase 12, ... | | Authors: | Kozicka, Z, Kempf, G, Focht, V, Thoma, N.H. | | Deposit date: | 2022-11-30 | | Release date: | 2023-09-13 | | Last modified: | 2024-03-27 | | Method: | X-RAY DIFFRACTION (3.26 Å) | | Cite: | Design principles for cyclin K molecular glue degraders.
Nat.Chem.Biol., 20, 2024
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8BUF
 | | Structure of DDB1 bound to Z12-engaged CDK12-cyclin K | | Descriptor: | 2-(6,7-dihydro-4~{H}-thieno[3,2-c]pyridin-5-ylmethyl)-6,7-dimethoxy-3~{H}-quinazolin-4-one, Cyclin-K, Cyclin-dependent kinase 12, ... | | Authors: | Kozicka, Z, Kempf, G, Petzold, G, Thoma, N.H. | | Deposit date: | 2022-11-30 | | Release date: | 2023-09-13 | | Last modified: | 2024-01-03 | | Method: | X-RAY DIFFRACTION (3.3 Å) | | Cite: | Design principles for cyclin K molecular glue degraders.
Nat.Chem.Biol., 20, 2024
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8BUA
 | | Structure of DDB1 bound to 919278-engaged CDK12-cyclin K | | Descriptor: | (2~{R})-~{N}-(1~{H}-benzimidazol-2-yl)-2-(3-oxidanylidene-1~{H}-isoindol-2-yl)propanamide, CITRIC ACID, Cyclin-K, ... | | Authors: | Kozicka, Z, Kempf, G, Petzold, G, Thoma, N.H. | | Deposit date: | 2022-11-30 | | Release date: | 2023-09-13 | | Last modified: | 2024-01-03 | | Method: | X-RAY DIFFRACTION (3.193 Å) | | Cite: | Design principles for cyclin K molecular glue degraders.
Nat.Chem.Biol., 20, 2024
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8BUO
 | | Structure of DDB1 bound to DS24-engaged CDK12-cyclin K | | Descriptor: | (2~{R})-2-[[6-[(3-fluoranyl-4-pyridin-2-yl-phenyl)methylamino]-9-propan-2-yl-purin-2-yl]amino]butan-1-ol, Cyclin-K, Cyclin-dependent kinase 12, ... | | Authors: | Kozicka, Z, Kempf, G, Petzold, G, Thoma, N.H. | | Deposit date: | 2022-11-30 | | Release date: | 2023-09-13 | | Last modified: | 2024-01-03 | | Method: | X-RAY DIFFRACTION (3.58 Å) | | Cite: | Design principles for cyclin K molecular glue degraders.
Nat.Chem.Biol., 20, 2024
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8BUD
 | | Structure of DDB1 bound to Z7-engaged CDK12-cyclin K | | Descriptor: | Cyclin-K, Cyclin-dependent kinase 12, DNA damage-binding protein 1, ... | | Authors: | Kozicka, Z, Kempf, G, Petzold, G, Thoma, N.H. | | Deposit date: | 2022-11-30 | | Release date: | 2023-09-13 | | Last modified: | 2024-01-03 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Design principles for cyclin K molecular glue degraders.
Nat.Chem.Biol., 20, 2024
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8BUG
 | | Structure of DDB1 bound to HQ461-engaged CDK12-cyclin K | | Descriptor: | 2-[2-[(6-methylpyridin-2-yl)amino]-1,3-thiazol-4-yl]-~{N}-(5-methyl-1,3-thiazol-2-yl)ethanamide, CITRIC ACID, Cyclin-K, ... | | Authors: | Kozicka, Z, Kempf, G, Focht, V, Thoma, N.H. | | Deposit date: | 2022-11-30 | | Release date: | 2023-09-13 | | Last modified: | 2024-03-27 | | Method: | X-RAY DIFFRACTION (3.53 Å) | | Cite: | Design principles for cyclin K molecular glue degraders.
Nat.Chem.Biol., 20, 2024
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8BU7
 | | Structure of DDB1 bound to 21195-engaged CDK12-cyclin K | | Descriptor: | 1,2-ETHANEDIOL, 1-[2,6-bis(chloranyl)phenyl]-6-[[4-(2-hydroxyethyloxy)phenyl]methyl]-3-propan-2-yl-5H-pyrazolo[3,4-d]pyrimidin-4-one, Cyclin-K, ... | | Authors: | Kozicka, Z, Kempf, G, Petzold, G, Thoma, N.H. | | Deposit date: | 2022-11-30 | | Release date: | 2023-09-13 | | Last modified: | 2024-01-03 | | Method: | X-RAY DIFFRACTION (3.245 Å) | | Cite: | Design principles for cyclin K molecular glue degraders.
Nat.Chem.Biol., 20, 2024
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8BU2
 | | Structure of DDB1 bound to DS18-engaged CDK12-cyclin K | | Descriptor: | Cyclin-K, Cyclin-dependent kinase 12, DNA damage-binding protein 1, ... | | Authors: | Kozicka, Z, Kempf, G, Petzold, G, Thoma, N.H. | | Deposit date: | 2022-11-30 | | Release date: | 2023-09-13 | | Last modified: | 2024-01-03 | | Method: | X-RAY DIFFRACTION (3.13 Å) | | Cite: | Design principles for cyclin K molecular glue degraders.
Nat.Chem.Biol., 20, 2024
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8BUE
 | | Structure of DDB1 bound to Z11-engaged CDK12-cyclin K | | Descriptor: | Cyclin-K, Cyclin-dependent kinase 12, DNA damage-binding protein 1, ... | | Authors: | Kozicka, Z, Kempf, G, Petzold, G, Thoma, N.H. | | Deposit date: | 2022-11-30 | | Release date: | 2023-09-13 | | Last modified: | 2024-01-03 | | Method: | X-RAY DIFFRACTION (3.25 Å) | | Cite: | Design principles for cyclin K molecular glue degraders.
Nat.Chem.Biol., 20, 2024
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8BU3
 | | Structure of DDB1 bound to DS19-engaged CDK12-cyclin K | | Descriptor: | 1,2-ETHANEDIOL, 2-morpholin-4-yl-9-propan-2-yl-~{N}-[(4-pyridin-2-ylphenyl)methyl]purin-6-amine, Cyclin-K, ... | | Authors: | Kozicka, Z, Kempf, G, Petzold, G, Thoma, N.H. | | Deposit date: | 2022-11-30 | | Release date: | 2023-09-13 | | Last modified: | 2024-01-03 | | Method: | X-RAY DIFFRACTION (3.42 Å) | | Cite: | Design principles for cyclin K molecular glue degraders.
Nat.Chem.Biol., 20, 2024
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8BUN
 | | Structure of DDB1 bound to DS16-engaged CDK12-cyclin K | | Descriptor: | (2~{R})-2-[[6-[(4-phenylphenyl)methylamino]-9-propan-2-yl-purin-2-yl]amino]butan-1-ol, Cyclin-K, Cyclin-dependent kinase 12, ... | | Authors: | Kozicka, Z, Kempf, G, Petzold, G, Thoma, N.H. | | Deposit date: | 2022-11-30 | | Release date: | 2023-09-13 | | Last modified: | 2024-01-03 | | Method: | X-RAY DIFFRACTION (3.08 Å) | | Cite: | Design principles for cyclin K molecular glue degraders.
Nat.Chem.Biol., 20, 2024
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8BUP
 | | Structure of DDB1 bound to DS30-engaged CDK12-cyclin K | | Descriptor: | (2~{R})-2-[[6-[3-(3-methylphenyl)propylamino]-9-propan-2-yl-purin-2-yl]amino]butan-1-ol, Cyclin-K, Cyclin-dependent kinase 12, ... | | Authors: | Kozicka, Z, Kempf, G, Petzold, G, Thoma, N.H. | | Deposit date: | 2022-11-30 | | Release date: | 2023-09-13 | | Last modified: | 2024-01-03 | | Method: | X-RAY DIFFRACTION (3.41 Å) | | Cite: | Design principles for cyclin K molecular glue degraders.
Nat.Chem.Biol., 20, 2024
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8BU4
 | | Structure of DDB1 bound to DS22-engaged CDK12-cyclin K | | Descriptor: | (2~{R})-2-[[6-[[5,6-bis(chloranyl)-1~{H}-benzimidazol-2-yl]methylamino]-9-(1-methylpyrazol-4-yl)purin-2-yl]amino]butan-1-ol, Cyclin-K, Cyclin-dependent kinase 12, ... | | Authors: | Kozicka, Z, Kempf, G, Focht, V, Thoma, N.H. | | Deposit date: | 2022-11-30 | | Release date: | 2023-09-13 | | Last modified: | 2024-03-27 | | Method: | X-RAY DIFFRACTION (3.09 Å) | | Cite: | Design principles for cyclin K molecular glue degraders.
Nat.Chem.Biol., 20, 2024
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8BUH
 | | Structure of DDB1 bound to WX3-engaged CDK12-cyclin K | | Descriptor: | 6-[[[2-[[(2~{R})-1-oxidanylbutan-2-yl]amino]-9-propan-2-yl-purin-6-yl]amino]methyl]-3-pyridin-2-yl-1~{H}-pyridin-2-one, Cyclin-K, Cyclin-dependent kinase 12, ... | | Authors: | Kozicka, Z, Kempf, G, Focht, V, Thoma, N.H. | | Deposit date: | 2022-11-30 | | Release date: | 2023-09-13 | | Last modified: | 2024-03-27 | | Method: | X-RAY DIFFRACTION (3.79 Å) | | Cite: | Design principles for cyclin K molecular glue degraders.
Nat.Chem.Biol., 20, 2024
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