4TTH
 
 | | Crystal structure of a CDK6/Vcyclin complex with inhibitor bound | | 分子名称: | 9-cyclopentyl-N-(5-piperazin-1-ylpyridin-2-yl)pyrido[4,5]pyrrolo[1,2-d]pyrimidin-2-amine, Cyclin homolog, Cyclin-dependent kinase 6 | | 著者 | Piper, D.E, Walker, N, Wang, Z. | | 登録日 | 2014-06-20 | | 公開日 | 2014-08-06 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.
J.Med.Chem., 57, 2014
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3TN8
 | | CDK9/cyclin T in complex with CAN508 | | 分子名称: | 4-[(E)-(3,5-DIAMINO-1H-PYRAZOL-4-YL)DIAZENYL]PHENOL, Cyclin-T1, Cyclin-dependent kinase 9, ... | | 著者 | Baumli, S, Hole, A.J, Endicott, J.E. | | 登録日 | 2011-09-01 | | 公開日 | 2012-02-15 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (2.95 Å) | | 主引用文献 | The CDK9 C-helix Exhibits Conformational Plasticity That May Explain the Selectivity of CAN508.
Acs Chem.Biol., 7, 2012
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3LQ5
 | | Structure of CDK9/CyclinT in complex with S-CR8 | | 分子名称: | (2S)-2-({9-(1-methylethyl)-6-[(4-pyridin-2-ylbenzyl)amino]-9H-purin-2-yl}amino)butan-1-ol, Cell division protein kinase 9, Cyclin-T1 | | 著者 | Hole, A.J, Endicott, J.A, Baumli, S. | | 登録日 | 2010-02-08 | | 公開日 | 2011-01-19 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | CDK Inhibitors Roscovitine and CR8 Trigger Mcl-1 Down-Regulation and Apoptotic Cell Death in Neuroblastoma Cells
Genes Cancer, 1, 2010
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3MI9
 | | Crystal structure of HIV-1 Tat complexed with human P-TEFb | | 分子名称: | Cell division protein kinase 9, Cyclin-T1, Protein Tat, ... | | 著者 | Tahirov, T.H, Babayeva, N.D, Varzavand, K, Cooper, J.J, Sedore, S.C, Price, D.H. | | 登録日 | 2010-04-09 | | 公開日 | 2010-06-09 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Crystal structure of HIV-1 Tat complexed with human P-TEFb.
Nature, 465, 2010
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3MIA
 | | Crystal structure of HIV-1 Tat complexed with ATP-bound human P-TEFb | | 分子名称: | Cell division protein kinase 9, Cyclin-T1, MAGNESIUM ION, ... | | 著者 | Tahirov, T.H, Babayeva, N.D, Varzavand, K, Cooper, J.J, Sedore, S.C, Price, D.H. | | 登録日 | 2010-04-09 | | 公開日 | 2010-06-09 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Crystal structure of HIV-1 Tat complexed with human P-TEFb.
Nature, 465, 2010
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3MY1
 | | Structure of CDK9/cyclinT1 in complex with DRB | | 分子名称: | 5,6-dichloro-1-beta-D-ribofuranosyl-1H-benzimidazole, Cell division protein kinase 9, Cyclin-T1, ... | | 著者 | Baumli, S, Johnson, L.N. | | 登録日 | 2010-05-09 | | 公開日 | 2010-09-29 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Halogen bonds form the basis for selective P-TEFb inhibition by DRB
Chem.Biol., 17, 2010
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3MY5
 | | CDk2/cyclinA in complex with DRB | | 分子名称: | 5,6-dichloro-1-beta-D-ribofuranosyl-1H-benzimidazole, Cell division protein kinase 2, Cyclin-A2, ... | | 著者 | Baumli, S, Johnson, L.N. | | 登録日 | 2010-05-09 | | 公開日 | 2010-09-29 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Halogen bonds form the basis for selective P-TEFb inhibition by DRB
Chem.Biol., 17, 2010
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6W9E
 | | Crystal Structure of Human CDK9/cyclinT1 in complex with MC180295 | | 分子名称: | (4-amino-2-{[(1R,2R,4S)-bicyclo[2.2.1]heptan-2-yl]amino}-1,3-thiazol-5-yl)(2-nitrophenyl)methanone, (4-amino-2-{[(1S,2S,4R)-bicyclo[2.2.1]heptan-2-yl]amino}-1,3-thiazol-5-yl)(2-nitrophenyl)methanone, Cyclin-T1, ... | | 著者 | Zhang, P, Wu, J. | | 登録日 | 2020-03-22 | | 公開日 | 2021-09-01 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Comparative Modeling of CDK9 Inhibitors to Explore Selectivity and Structure-Activity Relationships
To Be Published
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1VYW
 | | Structure of CDK2/Cyclin A with PNU-292137 | | 分子名称: | CELL DIVISION PROTEIN KINASE 2, CYCLIN A2, N-(3-CYCLOPROPYL-1H-PYRAZOL-5-YL)-2-(2-NAPHTHYL)ACETAMIDE, ... | | 著者 | Pevarello, P, Brasca, M.G, Amici, R, Orsini, P, Traquandi, G, Corti, L, Piutti, C, Sansonna, P, Villa, M, Pierce, B.S, Pulici, M, Giordano, P, Martina, K, Fritzen, E.L, Nugent, R.A, Casale, E, Cameron, A, Ciomei, M, Roletto, F, Isacchi, A, Fogliatto, G, Pesenti, E, Pastori, W, Marsiglio, A, Leach, K.L, Clare, P.M, Fiorentini, F, Varasi, M, Vulpetti, A, Warpehoski, M.A. | | 登録日 | 2004-05-07 | | 公開日 | 2004-06-10 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | 3-Aminopyrazole Inhibitors of Cdk2/Cyclin a as Antitumor Agents. Part 1. Lead Finding
J.Med.Chem., 47, 2004
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7ACK
 | | CDK2/cyclin A2 in complex with an imidazo[1,2-c]pyrimidin-5-one inhibitor | | 分子名称: | 1,2-ETHANEDIOL, 8-cyclohexyl-6~{H}-imidazo[1,2-c]pyrimidin-5-one, Cyclin-A2, ... | | 著者 | Skerlova, J, Pachl, P, Rezacova, P. | | 登録日 | 2020-09-11 | | 公開日 | 2021-03-24 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Imidazo[1,2-c]pyrimidin-5(6H)-one inhibitors of CDK2: Synthesis, kinase inhibition and co-crystal structure.
Eur.J.Med.Chem., 216, 2021
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1W98
 | | The structural basis of CDK2 activation by cyclin E | | 分子名称: | CELL DIVISION PROTEIN KINASE 2, G1/S-SPECIFIC CYCLIN E1 | | 著者 | Lowe, E.D, Honda, R, Dubinina, E, Skamnaki, V, Cook, A, Johnson, L.N. | | 登録日 | 2004-10-07 | | 公開日 | 2005-02-02 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2.15 Å) | | 主引用文献 | The Structure of Cyclin E1/Cdk2: Implications for Cdk2 Activation and Cdk2-Independent Roles
Embo J., 24, 2005
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7EGB
 | | TFIID-based holo PIC on SCP promoter | | 分子名称: | CDK-activating kinase assembly factor MAT1, Cyclin-H, Cyclin-dependent kinase 7, ... | | 著者 | Chen, X, Wu, Z, Hou, H, Qi, Y, Wang, X, Li, J, Xu, Y. | | 登録日 | 2021-03-24 | | 公開日 | 2021-05-05 | | 最終更新日 | 2023-07-26 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | Structural insights into preinitiation complex assembly on core promoters.
Science, 372, 2021
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7EGC
 | | p53-bound TFIID-based holo PIC on HDM2 promoter | | 分子名称: | CDK-activating kinase assembly factor MAT1, Cyclin-H, Cyclin-dependent kinase 7, ... | | 著者 | Chen, X, Wu, Z, Hou, H, Qi, Y, Wang, X, Li, J, Xu, Y. | | 登録日 | 2021-03-24 | | 公開日 | 2021-05-12 | | 実験手法 | ELECTRON MICROSCOPY (3.9 Å) | | 主引用文献 | Structural insights into preinitiation complex assembly on core promoters.
Science, 372, 2021
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7ENA
 | | TFIID-based PIC-Mediator holo-complex in pre-assembled state (pre-hPIC-MED) | | 分子名称: | CDK-activating kinase assembly factor MAT1, Cyclin-H, Cyclin-dependent kinase 7, ... | | 著者 | Chen, X, Qi, Y, Wang, X, Wu, Z, Yin, X, Li, J, Liu, W, Xu, Y. | | 登録日 | 2021-04-16 | | 公開日 | 2021-05-26 | | 最終更新日 | 2021-06-16 | | 実験手法 | ELECTRON MICROSCOPY (4.07 Å) | | 主引用文献 | Structures of the human Mediator and Mediator-bound preinitiation complex.
Science, 372, 2021
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7ENC
 | | TFIID-based PIC-Mediator holo-complex in fully-assembled state (hPIC-MED) | | 分子名称: | CDK-activating kinase assembly factor MAT1, Cyclin-H, Cyclin-dependent kinase 7, ... | | 著者 | Chen, X, Qi, Y, Wang, X, Wu, Z, Yin, X, Li, J, Liu, W, Xu, Y. | | 登録日 | 2021-04-16 | | 公開日 | 2021-05-26 | | 最終更新日 | 2021-06-16 | | 実験手法 | ELECTRON MICROSCOPY (4.13 Å) | | 主引用文献 | Structures of the human Mediator and Mediator-bound preinitiation complex.
Science, 372, 2021
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6XD3
 | | Structure of the human CAK in complex with THZ1 | | 分子名称: | CDK-activating kinase assembly factor MAT1, Cyclin-H, Cyclin-dependent kinase 7, ... | | 著者 | Greber, B.J, Perez-Bertoldi, J.M, Lim, K, Iavarone, A.T, Toso, D.B, Nogales, E. | | 登録日 | 2020-06-09 | | 公開日 | 2020-09-09 | | 最終更新日 | 2020-09-30 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | The cryoelectron microscopy structure of the human CDK-activating kinase.
Proc.Natl.Acad.Sci.USA, 117, 2020
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6XBZ
 | | Structure of the human CDK-activating kinase | | 分子名称: | CDK-activating kinase assembly factor MAT1, Cyclin-H, Cyclin-dependent kinase 7, ... | | 著者 | Greber, B.J, Perez-Bertoldi, J.M, Lim, K, Iavarone, A.T, Toso, D.B, Nogales, E. | | 登録日 | 2020-06-07 | | 公開日 | 2020-09-09 | | 最終更新日 | 2020-09-30 | | 実験手法 | ELECTRON MICROSCOPY (2.8 Å) | | 主引用文献 | The cryoelectron microscopy structure of the human CDK-activating kinase.
Proc.Natl.Acad.Sci.USA, 117, 2020
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7B5Q
 | | Cryo-EM structure of the human CAK bound to ICEC0942 (PHENIX-OPLS3e) | | 分子名称: | (3R,4R)-4-[[[7-[(phenylmethyl)amino]-3-propan-2-yl-pyrazolo[1,5-a]pyrimidin-5-yl]amino]methyl]piperidin-3-ol, CDK-activating kinase assembly factor MAT1, Cyclin-H, ... | | 著者 | Greber, B.J, Remis, J, Ali, S, Nogales, E. | | 登録日 | 2020-12-05 | | 公開日 | 2021-02-10 | | 最終更新日 | 2024-05-15 | | 実験手法 | ELECTRON MICROSCOPY (2.5 Å) | | 主引用文献 | 2.5 angstrom -resolution structure of human CDK-activating kinase bound to the clinical inhibitor ICEC0942.
Biophys.J., 120, 2021
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7B5O
 | | Cryo-EM structure of the human CAK bound to ICEC0942 at 2.5 Angstroms resolution | | 分子名称: | (3R,4R)-4-[[[7-[(phenylmethyl)amino]-3-propan-2-yl-pyrazolo[1,5-a]pyrimidin-5-yl]amino]methyl]piperidin-3-ol, CDK-activating kinase assembly factor MAT1, Cyclin-H, ... | | 著者 | Greber, B.J, Remis, J, Ali, S, Nogales, E. | | 登録日 | 2020-12-05 | | 公開日 | 2021-02-10 | | 最終更新日 | 2024-05-01 | | 実験手法 | ELECTRON MICROSCOPY (2.5 Å) | | 主引用文献 | 2.5 angstrom -resolution structure of human CDK-activating kinase bound to the clinical inhibitor ICEC0942.
Biophys.J., 120, 2021
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7B5R
 | | Ubiquitin ligation to F-box protein substrates by SCF-RBR E3-E3 super-assembly: CUL1-RBX1-SKP1-SKP2-CKSHS1-Cyclin A-CDK2-p27 | | 分子名称: | Cullin-1, Cyclin-A2, Cyclin-dependent kinase 2, ... | | 著者 | Horn-Ghetko, D, Prabu, J.R, Schulman, B.A. | | 登録日 | 2020-12-07 | | 公開日 | 2021-02-10 | | 最終更新日 | 2021-03-10 | | 実験手法 | ELECTRON MICROSCOPY (3.8 Å) | | 主引用文献 | Ubiquitin ligation to F-box protein targets by SCF-RBR E3-E3 super-assembly.
Nature, 590, 2021
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7B5L
 | | Ubiquitin ligation to F-box protein substrates by SCF-RBR E3-E3 super-assembly: NEDD8-CUL1-RBX1-SKP1-SKP2-CKSHS1-Cyclin A-CDK2-p27-UBE2L3~Ub~ARIH1. Transition State 1 | | 分子名称: | 5-azanylpentan-2-one, Cullin-1, Cyclin-A2, ... | | 著者 | Horn-Ghetko, D, Prabu, J.R, Schulman, B.A. | | 登録日 | 2020-12-04 | | 公開日 | 2021-02-10 | | 最終更新日 | 2021-03-10 | | 実験手法 | ELECTRON MICROSCOPY (3.8 Å) | | 主引用文献 | Ubiquitin ligation to F-box protein targets by SCF-RBR E3-E3 super-assembly.
Nature, 590, 2021
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6XI8
 | | Yeast TFIIK (Kin28/Ccl1/Tfb3) Complex | | 分子名称: | ADENOSINE-5'-DIPHOSPHATE, ALUMINUM FLUORIDE, Cyclin CCL1, ... | | 著者 | van Eeuwen, T, Murakami, K, Li, T, Tsai, K.L. | | 登録日 | 2020-06-19 | | 公開日 | 2021-04-28 | | 実験手法 | ELECTRON MICROSCOPY (3.64 Å) | | 主引用文献 | Structure of TFIIK for phosphorylation of CTD of RNA polymerase II.
Sci Adv, 7, 2021
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7B7S
 | | CDK2/cyclin A2 in complex with 3H-pyrazolo[4,3-f]quinoline-based derivative HSD1368 | | 分子名称: | 7-(3-(trifluoromethyl)-1H-pyrazol-4yl)-3,8,10,11-tetrahydropyrazolo[4,3-f]thiopyrano[3,4-c]quinoline 9-oxide, Cyclin-A2, Cyclin-dependent kinase 2, ... | | 著者 | Djukic, S, Skerlova, J, Rezacova, P. | | 登録日 | 2020-12-11 | | 公開日 | 2021-08-04 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (2.54 Å) | | 主引用文献 | 3 H -Pyrazolo[4,3- f ]quinoline-Based Kinase Inhibitors Inhibit the Proliferation of Acute Myeloid Leukemia Cells In Vivo.
J.Med.Chem., 64, 2021
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1XO2
 | | Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin | | 分子名称: | 3,7,3',4'-TETRAHYDROXYFLAVONE, Cell division protein kinase 6, Cyclin | | 著者 | Lu, H.S, Chang, D.J, Baratte, B, Meijer, L, Schulze-Gahmen, U. | | 登録日 | 2004-10-05 | | 公開日 | 2005-03-01 | | 最終更新日 | 2023-08-23 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | Crystal Structure of a Human Cyclin-Dependent Kinase 6 Complex with a Flavonol Inhibitor, Fisetin.
J.Med.Chem., 48, 2005
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6Y0A
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