7KPV
 
 | | Structure of kinase and Central lobes of yeast CKM | | Descriptor: | Mediator of RNA polymerase II transcription subunit 12, Mediator of RNA polymerase II transcription subunit 13, Meiotic mRNA stability protein kinase SSN3, ... | | Authors: | Li, Y.C, Chao, T.C, Kim, H.J, Cholko, T, Chen, S.F, Nakanishi, K, Chang, C.E, Murakami, K, Garcia, B.A, Boyer, T.G, Tsai, K.L. | | Deposit date: | 2020-11-12 | | Release date: | 2021-01-27 | | Last modified: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (3.8 Å) | | Cite: | Structure and noncanonical Cdk8 activation mechanism within an Argonaute-containing Mediator kinase module.
Sci Adv, 7, 2021
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7LBM
 | | Structure of the human Mediator-bound transcription pre-initiation complex | | Descriptor: | CDK-activating kinase assembly factor MAT1, Cyclin-H, Cyclin-dependent kinase 7, ... | | Authors: | Abdella, R, Talyzina, A, He, Y. | | Deposit date: | 2021-01-08 | | Release date: | 2021-03-24 | | Last modified: | 2021-04-14 | | Method: | ELECTRON MICROSCOPY (4.8 Å) | | Cite: | Structure of the human Mediator-bound transcription preinitiation complex.
Science, 372, 2021
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7KUE
 | | CryoEM structure of Yeast TFIIK (Kin28/Ccl1/Tfb3) Complex | | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, ALUMINUM FLUORIDE, Cyclin CCL1, ... | | Authors: | van Eeuwen, T, Murakami, K, Li, T, Tsai, K.L. | | Deposit date: | 2020-11-24 | | Release date: | 2021-04-28 | | Method: | ELECTRON MICROSCOPY (3.5 Å) | | Cite: | Structure of TFIIK for phosphorylation of CTD of RNA polymerase II.
Sci Adv, 7, 2021
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1XO2
 | | Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin | | Descriptor: | 3,7,3',4'-TETRAHYDROXYFLAVONE, Cell division protein kinase 6, Cyclin | | Authors: | Lu, H.S, Chang, D.J, Baratte, B, Meijer, L, Schulze-Gahmen, U. | | Deposit date: | 2004-10-05 | | Release date: | 2005-03-01 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Crystal Structure of a Human Cyclin-Dependent Kinase 6 Complex with a Flavonol Inhibitor, Fisetin.
J.Med.Chem., 48, 2005
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5CEI
 | | Crystal structure of CDK8:Cyclin C complex with compound 22 | | Descriptor: | 1,2-ETHANEDIOL, 4-(4-iodophenoxy)-N-methylthieno[2,3-c]pyridine-2-carboxamide, Cyclin-C, ... | | Authors: | Kiefer, J.R, Schneider, E.V, Maskos, K, Koehler, M.F.T. | | Deposit date: | 2015-07-06 | | Release date: | 2016-02-10 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (2.24 Å) | | Cite: | Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells.
Acs Med.Chem.Lett., 7, 2016
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5CYI
 | | CDK2/Cyclin A covalent complex with 6-(cyclohexylmethoxy)-N-(4-(vinylsulfonyl)phenyl)-9H-purin-2-amine (NU6300) | | Descriptor: | 6-(cyclohexylmethoxy)-N-[4-(ethylsulfonyl)phenyl]-9H-purin-2-amine, Cyclin-A2, Cyclin-dependent kinase 2 | | Authors: | Anscombe, E, Meschini, E, Vidal, R.M, Martin, M.P, Staunton, D, Geitmann, M, Danielson, U.H, Stanley, W.A, Wang, L.Z, Reuillon, T, Golding, B.T, Cano, C, Newell, D.R, Noble, M.E.M, Wedge, S.R, Endicott, J.A, Griffin, R.J. | | Deposit date: | 2015-07-30 | | Release date: | 2015-09-16 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Identification and Characterization of an Irreversible Inhibitor of CDK2.
Chem.Biol., 22, 2015
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6O9L
 | | Human holo-PIC in the closed state | | Descriptor: | CDK-activating kinase assembly factor MAT1, Cyclin-H, Cyclin-dependent kinase 7, ... | | Authors: | Yan, C.L, Dodd, T, He, Y, Tainer, J.A, Tsutakawa, S.E, Ivanov, I. | | Deposit date: | 2019-03-14 | | Release date: | 2019-05-29 | | Last modified: | 2024-03-13 | | Method: | ELECTRON MICROSCOPY (7.2 Å) | | Cite: | Transcription preinitiation complex structure and dynamics provide insight into genetic diseases.
Nat.Struct.Mol.Biol., 26, 2019
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6P3W
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6P8F
 | | Crystal structure of CDK4 in complex with CyclinD1 and P27 | | Descriptor: | Cyclin-dependent kinase 4, Cyclin-dependent kinase inhibitor 1B, G1/S-specific cyclin-D1 | | Authors: | Guiley, K.Z, Stevenson, J.W, Lou, K, Barkovich, K.J, Bunch, K, Tripathi, S.M, Shokat, K.M, Rubin, S.M. | | Deposit date: | 2019-06-07 | | Release date: | 2019-12-25 | | Method: | X-RAY DIFFRACTION (2.89 Å) | | Cite: | p27 allosterically activates cyclin-dependent kinase 4 and antagonizes palbociclib inhibition.
Science, 366, 2019
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7MKX
 | | Crystal Structure Analysis of human CDK2 and CCNA2 complex | | Descriptor: | 2-[(5-bromo-2-{4-[(cyanomethyl)sulfamoyl]anilino}pyrimidin-4-yl)amino]-6-fluorobenzamide, Cyclin-A2, Cyclin-dependent kinase 2 | | Authors: | Seo, H.-S, Dhe-Paganon, S. | | Deposit date: | 2021-04-27 | | Release date: | 2022-11-09 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (3.08 Å) | | Cite: | Crystal Structure Analysis of human CDK2 and CCNA2 complex
To Be Published
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6P8H
 | | Crystal structure of CDK4 in complex with CyclinD1 and P21 | | Descriptor: | Cyclin-dependent kinase 4, Cyclin-dependent kinase inhibitor 1, G1/S-specific cyclin-D1 | | Authors: | Guiley, K.Z, Stevenson, J.W, Lou, K, Barkovich, K.J, Bunch, K, Tripathi, S.M, Shokat, K.M, Rubin, S.M. | | Deposit date: | 2019-06-07 | | Release date: | 2019-12-25 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3.19 Å) | | Cite: | p27 allosterically activates cyclin-dependent kinase 4 and antagonizes palbociclib inhibition.
Science, 366, 2019
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7NVR
 | | Human Mediator with RNA Polymerase II Pre-initiation complex | | Descriptor: | CDK-activating kinase assembly factor MAT1, Cyclin-H, Cyclin-dependent kinase 7, ... | | Authors: | Rengachari, S, Schilbach, S, Aibara, S, Cramer, P. | | Deposit date: | 2021-03-15 | | Release date: | 2021-05-05 | | Last modified: | 2021-06-16 | | Method: | ELECTRON MICROSCOPY (4.5 Å) | | Cite: | Structures of mammalian RNA polymerase II pre-initiation complexes.
Nature, 594, 2021
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7NXJ
 | | Crystal structure of human Cdk13/Cyclin K in complex with the inhibitor THZ531 | | Descriptor: | Cyclin-K, Cyclin-dependent kinase 13, N-[4-[(3R)-3-[[5-chloranyl-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]piperidin-1-yl]carbonylphenyl]-4-(dimethylamino)butanamide | | Authors: | Anand, K, Greifenberg, A.K, Kaltheuner, I.H, Geyer, M. | | Deposit date: | 2021-03-18 | | Release date: | 2021-05-12 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2.36 Å) | | Cite: | Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma.
Eur.J.Med.Chem., 221, 2021
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7NXK
 | | Crystal structure of human Cdk12/Cyclin K in complex with the inhibitor BSJ-01-175 | | Descriptor: | (E)-N-[4-[(1R,3R)-3-[[5-chloranyl-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]cyclohexyl]oxyphenyl]-4-(dimethylamino)but-2-enamide, Cyclin-K, Cyclin-dependent kinase 12 | | Authors: | Anand, K, Dust, S, Kaltheuner, I.H, Geyer, M. | | Deposit date: | 2021-03-18 | | Release date: | 2021-05-12 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma.
Eur.J.Med.Chem., 221, 2021
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6P8G
 | | Crystal structure of CDK4 in complex with CyclinD1 and P27 | | Descriptor: | Cyclin-dependent kinase 4, Cyclin-dependent kinase inhibitor 1B, G1/S-specific cyclin-D1 | | Authors: | Guiley, K.Z, Stevenson, J.W, Lou, K, Barkovich, K.J, Bunch, K, Tripathi, S.M, Shokat, K.M, Rubin, S.M. | | Deposit date: | 2019-06-07 | | Release date: | 2019-12-25 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | p27 allosterically activates cyclin-dependent kinase 4 and antagonizes palbociclib inhibition.
Science, 366, 2019
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7NJ0
 | | CryoEM structure of the human Separase-Cdk1-cyclin B1-Cks1 complex | | Descriptor: | Cyclin-dependent kinase 1, Cyclin-dependent kinases regulatory subunit 1, G2/mitotic-specific cyclin-B1,G2/mitotic-specific cyclin-B1, ... | | Authors: | Yu, J, Raia, P, Ghent, C.M, Raisch, T, Sadian, Y, Barford, D, Raunser, S, Morgan, D.O, Boland, A. | | Deposit date: | 2021-02-14 | | Release date: | 2021-08-04 | | Last modified: | 2021-08-18 | | Method: | ELECTRON MICROSCOPY (3.6 Å) | | Cite: | Structural basis of human separase regulation by securin and CDK1-cyclin B1.
Nature, 596, 2021
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6P8E
 | | Crystal structure of CDK4 in complex with CyclinD1 and P27 | | Descriptor: | Cyclin-dependent kinase 4, Cyclin-dependent kinase inhibitor 1B, G1/S-specific cyclin-D1, ... | | Authors: | Guiley, K.Z, Stevenson, J.W, Lou, K, Barkovich, K.J, Bunch, K, Tripathi, S.M, Shokat, K.M, Rubin, S.M. | | Deposit date: | 2019-06-07 | | Release date: | 2019-12-25 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | p27 allosterically activates cyclin-dependent kinase 4 and antagonizes palbociclib inhibition.
Science, 366, 2019
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7NWK
 | | Crystal structure of CDK9-Cyclin T1 bound by compound 6 | | Descriptor: | Cyclin-T1, Cyclin-dependent kinase 9, N-((1R,3R)-3-(7-(4-fluoro-2-methoxyphenyl)-3H-imidazo[4,5-b]pyridin-2-yl)cyclopentyl)acetamide | | Authors: | Collie, G.W, Ferguson, A.D. | | Deposit date: | 2021-03-16 | | Release date: | 2021-10-27 | | Last modified: | 2021-11-10 | | Method: | X-RAY DIFFRACTION (2.81 Å) | | Cite: | Discovery of a Series of 7-Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement.
J.Med.Chem., 64, 2021
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2UUE
 | | REPLACE: A strategy for Iterative Design of Cyclin Binding Groove Inhibitors | | Descriptor: | 1-(3,5-DICHLOROPHENYL)-5-METHYL-1H-1,2,4-TRIAZOLE-3-CARBOXYLIC ACID, 4-METHYL-5-{(2E)-2-[(4-MORPHOLIN-4-YLPHENYL)IMINO]-2,5-DIHYDROPYRIMIDIN-4-YL}-1,3-THIAZOL-2-AMINE, CELL DIVISION PROTEIN KINASE 2, ... | | Authors: | Andrews, M.J, Kontopidis, G, McInnes, C, Plater, A, Innes, L, Cowan, A, Jewsbury, P, Fischer, P.M. | | Deposit date: | 2007-03-02 | | Release date: | 2007-03-27 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.06 Å) | | Cite: | Replace: A Strategy for Iterative Design of Cyclin- Binding Groove Inhibitors
Chembiochem, 7, 2006
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2UZB
 | | Crystal structure of human CDK2 complexed with a thiazolidinone inhibitor | | Descriptor: | 4-{5-[(Z)-(2-IMINO-4-OXO-1,3-THIAZOLIDIN-5-YLIDENE)METHYL]-2-FURYL}-N-METHYLBENZENESULFONAMIDE, CELL DIVISION PROTEIN KINASE 2, CYCLIN-A2 | | Authors: | Richardson, C.M, Dokurno, P, Murray, J.B, Surgenor, A.E. | | Deposit date: | 2007-04-27 | | Release date: | 2007-06-26 | | Last modified: | 2019-04-03 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Discovery of a Potent Cdk2 Inhibitor with a Novel Binding Mode, Using Virtual Screening and Initial, Structure-Guided Lead Scoping.
Bioorg.Med.Chem.Lett., 17, 2007
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2UZD
 | | Crystal structure of human CDK2 complexed with a thiazolidinone inhibitor | | Descriptor: | 4-{5-[(Z)-(2-IMINO-4-OXO-1,3-THIAZOLIDIN-5-YLIDENE)METHYL]FURAN-2-YL}BENZENESULFONAMIDE, CELL DIVISION PROTEIN KINASE 2, CYCLIN A2 | | Authors: | Richardson, C.M, Dokurno, P, Murray, J.B, Surgenor, A.E. | | Deposit date: | 2007-04-27 | | Release date: | 2007-06-26 | | Last modified: | 2019-04-03 | | Method: | X-RAY DIFFRACTION (2.72 Å) | | Cite: | Discovery of a Potent Cdk2 Inhibitor with a Novel Binding Mode, Using Virtual Screening and Initial, Structure-Guided Lead Scoping.
Bioorg.Med.Chem.Lett., 17, 2007
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2UZE
 | | Crystal structure of human CDK2 complexed with a thiazolidinone inhibitor | | Descriptor: | 4-{5-[(Z)-(2-IMINO-4-OXO-1,3-THIAZOLIDIN-5-YLIDENE)METHYL]FURAN-2-YL}BENZOIC ACID, CELL DIVISION PROTEIN KINASE 2, CYCLIN A2 | | Authors: | Richardson, C.M, Dokurno, P, Murray, J.B, Surgenor, A.E. | | Deposit date: | 2007-04-27 | | Release date: | 2007-06-26 | | Last modified: | 2019-04-03 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Discovery of a Potent Cdk2 Inhibitor with a Novel Binding Mode, Using Virtual Screening and Initial, Structure-Guided Lead Scoping.
Bioorg.Med.Chem.Lett., 17, 2007
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2UZL
 | | Crystal structure of human CDK2 complexed with a thiazolidinone inhibitor | | Descriptor: | 4-{5-[(Z)-(2-IMINO-4-OXO-1,3-THIAZOLIDIN-5-YLIDENE)METHYL]FURAN-2-YL}-2-(TRIFLUOROMETHYL)BENZENESULFONAMIDE, CELL DIVISION PROTEIN KINASE 2, CYCLIN A2 | | Authors: | Richardson, C.M, Dokurno, P, Murray, J.B, Surgenor, A.E. | | Deposit date: | 2007-04-30 | | Release date: | 2007-06-26 | | Last modified: | 2019-04-03 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Discovery of a Potent Cdk2 Inhibitor with a Novel Binding Mode, Using Virtual Screening and Initial, Structure-Guided Lead Scoping.
Bioorg.Med.Chem.Lett., 17, 2007
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2V22
 | | REPLACE: A strategy for Iterative Design of Cyclin Binding Groove Inhibitors | | Descriptor: | CELL DIVISION PROTEIN KINASE 2, CYCLIN-A2, N~2~-{[1-(4-CHLOROPHENYL)-5-METHYL-1H-1,2,4-TRIAZOL-3-YL]CARBONYL}-N~5~-(DIAMINOMETHYLIDENE)-L-ORNITHYL-L-LEUCYL-L-ISOLEUCYL-4-FLUORO-L-PHENYLALANINAMIDE | | Authors: | Andrews, M.J, Kontopidis, G, McInnes, C, Plater, A, Innes, L, Cowan, A, Jewsbury, P, Fischer, P.M. | | Deposit date: | 2007-05-31 | | Release date: | 2008-01-29 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Replace: A Strategy for Iterative Design of Cyclin- Binding Groove Inhibitors
Chembiochem, 7, 2006
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2G9X
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