2XAQ
 
 | | Crystal structure of LSD1-CoREST in complex with a tranylcypromine derivative (MC2584, 13b) | | 分子名称: | 3-{4-[(PHENYLCARBONYL)AMINO]PHENYL}PROPANOIC ACID, FLAVIN-ADENINE DINUCLEOTIDE, LYSINE-SPECIFIC HISTONE DEMETHYLASE 1, ... | | 著者 | Binda, C, Valente, S, Romanenghi, M, Pilotto, S, Cirilli, R, Karytinos, A, Ciossani, G, Botrugno, O.A, Forneris, F, Tardugno, M, Edmondson, D.E, Minucci, S, Mattevi, A, Mai, A. | | 登録日 | 2010-03-31 | | 公開日 | 2010-05-05 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Biochemical, Structural, and Biological Evaluation of Tranylcypromine Derivatives as Inhibitors of Histone Demethylases Lsd1 and Lsd2.
J.Am.Chem.Soc., 132, 2010
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1M7Q
 | | Crystal structure of p38 MAP kinase in complex with a dihydroquinazolinone inhibitor | | 分子名称: | 1-(2,6-DICHLOROPHENYL)-5-(2,4-DIFLUOROPHENYL)-7-PIPERAZIN-1-YL-3,4-DIHYDROQUINAZOLIN-2(1H)-ONE, Mitogen-activated protein kinase 14, SULFATE ION | | 著者 | Stelmach, J.E, Liu, L, Patel, S.B, Pivnichny, J.V, Scapin, G, Singh, S, Hop, C.E.C.A, Wang, Z, Cameron, P.M, Nichols, E.A, O'Keefe, S.J, O'Neill, E.A, Schmatz, D.M, Schwartz, C.D, Thompson, C.M, Zaller, D.M, Doherty, J.B. | | 登録日 | 2002-07-22 | | 公開日 | 2002-12-11 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.
Bioorg.Med.Chem.Lett., 13, 2003
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6GU3
 | | CDK1/CyclinB/Cks2 in complex with AZD5438 | | 分子名称: | 4-(2-methyl-3-propan-2-yl-imidazol-4-yl)-~{N}-(4-methylsulfonylphenyl)pyrimidin-2-amine, Cyclin-dependent kinase 1, Cyclin-dependent kinases regulatory subunit 2, ... | | 著者 | Wood, D.J, Korolchuk, S, Tatum, N.J, Wang, L.Z, Endicott, J.A, Noble, M.E.M, Martin, M.P. | | 登録日 | 2018-06-19 | | 公開日 | 2018-12-05 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.65 Å) | | 主引用文献 | Differences in the Conformational Energy Landscape of CDK1 and CDK2 Suggest a Mechanism for Achieving Selective CDK Inhibition.
Cell Chem Biol, 26, 2019
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2XAG
 | | Crystal structure of LSD1-CoREST in complex with para-bromo-(-)-trans- 2-phenylcyclopropyl-1-amine | | 分子名称: | 3-(4-BROMOPHENYL)PROPANAMIDE, FLAVIN-ADENINE DINUCLEOTIDE, LYSINE-SPECIFIC HISTONE DEMETHYLASE 1, ... | | 著者 | Binda, C, Valente, S, Romanenghi, M, Pilotto, S, Cirilli, R, Karytinos, A, Ciossani, G, Botrugno, O.A, Forneris, F, Tardugno, M, Edmondson, D.E, Minucci, S, Mattevi, A, Mai, A. | | 登録日 | 2010-03-31 | | 公開日 | 2010-05-05 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Biochemical, Structural, and Biological Evaluation of Tranylcypromine Derivatives as Inhibitors of Histone Demethylases Lsd1 and Lsd2.
J.Am.Chem.Soc., 132, 2010
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2XAJ
 | | Crystal structure of LSD1-CoREST in complex with (-)-trans-2- phenylcyclopropyl-1-amine | | 分子名称: | FLAVIN-ADENINE DINUCLEOTIDE, LYSINE-SPECIFIC HISTONE DEMETHYLASE 1, PHENYLETHYLENECARBOXYLIC ACID, ... | | 著者 | Binda, C, Valente, S, Romanenghi, M, Pilotto, S, Cirilli, R, Karytinos, A, Ciossani, G, Botrugno, O.A, Forneris, F, Tardugno, M, Edmondson, D.E, Minucci, S, Mattevi, A, Mai, A. | | 登録日 | 2010-03-31 | | 公開日 | 2010-05-05 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (3.3 Å) | | 主引用文献 | Biochemical, Structural, and Biological Evaluation of Tranylcypromine Derivatives as Inhibitors of Histone Demethylases Lsd1 and Lsd2.
J.Am.Chem.Soc., 132, 2010
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3HV5
 | | Human p38 MAP Kinase in Complex with RL24 | | 分子名称: | 1-[3-tert-butyl-1-(4-methylphenyl)-1H-pyrazol-5-yl]-3-{3-[(6-nitroquinolin-4-yl)amino]phenyl}urea, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Mitogen-activated protein kinase 14, ... | | 著者 | Gruetter, C, Simard, J.R, Getlik, M, Rauh, D. | | 登録日 | 2009-06-15 | | 公開日 | 2009-11-17 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.25 Å) | | 主引用文献 | Displacement assay for the detection of stabilizers of inactive kinase conformations.
J.Med.Chem., 53, 2010
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2ZB0
 | | Crystal structure of P38 in complex with biphenyl amide inhibitor | | 分子名称: | GLYCEROL, Mitogen-activated protein kinase 14, N-(3-cyanophenyl)-2'-methyl-5'-(5-methyl-1,3,4-oxadiazol-2-yl)-4-biphenylcarboxamide | | 著者 | Somers, D.O. | | 登録日 | 2007-10-13 | | 公開日 | 2008-01-15 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Biphenyl amide p38 kinase inhibitors 1: Discovery and binding mode
Bioorg.Med.Chem.Lett., 18, 2008
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3K3I
 | | p38alpha bound to novel DGF-out compound PF-00215955 | | 分子名称: | (3S)-3-[4-(4-bromophenyl)-1H-imidazol-2-yl]-1,2,3,4-tetrahydroisoquinoline, 2-fluoro-4-[4-(4-fluorophenyl)-1H-pyrazol-3-yl]pyridine, Mitogen-activated protein kinase 14 | | 著者 | Kazmirski, S.L, DiNitto, J.P. | | 登録日 | 2009-10-02 | | 公開日 | 2009-11-17 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | | 主引用文献 | The design, synthesis and potential utility of fluorescence probes that target DFG-out conformation of p38alpha for high throughput screening binding assay.
Chem.Biol.Drug Des., 74, 2009
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7W3B
 | | Structure of USP14-bound human 26S proteasome in substrate-engaged state ED5_USP14 | | 分子名称: | 26S protease regulatory subunit 4, 26S protease regulatory subunit 6A, 26S protease regulatory subunit 6B, ... | | 著者 | Zhang, S, Zou, S, Yin, D, Wu, Z, Mao, Y. | | 登録日 | 2021-11-25 | | 公開日 | 2022-05-04 | | 最終更新日 | 2022-06-01 | | 実験手法 | ELECTRON MICROSCOPY (3.6 Å) | | 主引用文献 | USP14-regulated allostery of the human proteasome by time-resolved cryo-EM.
Nature, 605, 2022
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7W3G
 | | Structure of USP14-bound human 26S proteasome in substrate-engaged state ED2.0_USP14 | | 分子名称: | 26S protease regulatory subunit 4, 26S protease regulatory subunit 6A, 26S protease regulatory subunit 6B, ... | | 著者 | Zhang, S, Zou, S, Yin, D, Wu, Z, Mao, Y. | | 登録日 | 2021-11-25 | | 公開日 | 2022-05-04 | | 最終更新日 | 2022-06-01 | | 実験手法 | ELECTRON MICROSCOPY (3.2 Å) | | 主引用文献 | USP14-regulated allostery of the human proteasome by time-resolved cryo-EM.
Nature, 605, 2022
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7W3J
 | | Structure of USP14-bound human 26S proteasome in substrate-inhibited state SC_USP14 | | 分子名称: | 26S protease regulatory subunit 4, 26S protease regulatory subunit 6A, 26S protease regulatory subunit 6B, ... | | 著者 | Zhang, S, Zou, S, Yin, D, Wu, Z, Mao, Y. | | 登録日 | 2021-11-25 | | 公開日 | 2022-05-04 | | 最終更新日 | 2022-06-01 | | 実験手法 | ELECTRON MICROSCOPY (3.5 Å) | | 主引用文献 | USP14-regulated allostery of the human proteasome by time-resolved cryo-EM.
Nature, 605, 2022
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7W3C
 | | Structure of USP14-bound human 26S proteasome in substrate-engaged state ED0_USP14 | | 分子名称: | 26S protease regulatory subunit 4, 26S protease regulatory subunit 6A, 26S protease regulatory subunit 6B, ... | | 著者 | Zhang, S, Zou, S, Yin, D, Wu, Z, Mao, Y. | | 登録日 | 2021-11-25 | | 公開日 | 2022-05-04 | | 最終更新日 | 2022-06-01 | | 実験手法 | ELECTRON MICROSCOPY (3.4 Å) | | 主引用文献 | USP14-regulated allostery of the human proteasome by time-resolved cryo-EM.
Nature, 605, 2022
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7W3A
 | | Structure of USP14-bound human 26S proteasome in substrate-engaged state ED4_USP14 | | 分子名称: | 26S protease regulatory subunit 4, 26S protease regulatory subunit 6A, 26S protease regulatory subunit 6B, ... | | 著者 | Zhang, S, Zou, S, Yin, D, Wu, Z, Mao, Y. | | 登録日 | 2021-11-25 | | 公開日 | 2022-05-04 | | 最終更新日 | 2022-06-01 | | 実験手法 | ELECTRON MICROSCOPY (3.5 Å) | | 主引用文献 | USP14-regulated allostery of the human proteasome by time-resolved cryo-EM.
Nature, 605, 2022
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7W3F
 | | Structure of USP14-bound human 26S proteasome in substrate-engaged state ED1_USP14 | | 分子名称: | 26S protease regulatory subunit 4, 26S protease regulatory subunit 6A, 26S protease regulatory subunit 6B, ... | | 著者 | Zhang, S, Zou, S, Yin, D, Wu, Z, Mao, Y. | | 登録日 | 2021-11-25 | | 公開日 | 2022-05-04 | | 最終更新日 | 2022-06-01 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | USP14-regulated allostery of the human proteasome by time-resolved cryo-EM.
Nature, 605, 2022
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7W37
 | | Structure of USP14-bound human 26S proteasome in state EA1_UBL | | 分子名称: | 26S protease regulatory subunit 4, 26S protease regulatory subunit 6A, 26S protease regulatory subunit 6B, ... | | 著者 | Zhang, S, Zou, S, Yin, D, Wu, Z, Mao, Y. | | 登録日 | 2021-11-25 | | 公開日 | 2022-05-04 | | 最終更新日 | 2022-06-01 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | USP14-regulated allostery of the human proteasome by time-resolved cryo-EM.
Nature, 605, 2022
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7W38
 | | Structure of USP14-bound human 26S proteasome in state EA2.0_UBL | | 分子名称: | 26S protease regulatory subunit 4, 26S protease regulatory subunit 6A, 26S protease regulatory subunit 6B, ... | | 著者 | Zhang, S, Zou, S, Yin, D, Wu, Z, Mao, Y. | | 登録日 | 2021-11-25 | | 公開日 | 2022-05-04 | | 最終更新日 | 2022-06-01 | | 実験手法 | ELECTRON MICROSCOPY (3.1 Å) | | 主引用文献 | USP14-regulated allostery of the human proteasome by time-resolved cryo-EM.
Nature, 605, 2022
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7W3K
 | | Structure of USP14-bound human 26S proteasome in substrate-inhibited state SD4_USP14 | | 分子名称: | 26S protease regulatory subunit 4, 26S protease regulatory subunit 6A, 26S protease regulatory subunit 6B, ... | | 著者 | Zhang, S, Zou, S, Yin, D, Wu, Z, Mao, Y. | | 登録日 | 2021-11-25 | | 公開日 | 2022-05-04 | | 最終更新日 | 2022-06-01 | | 実験手法 | ELECTRON MICROSCOPY (3.6 Å) | | 主引用文献 | USP14-regulated allostery of the human proteasome by time-resolved cryo-EM.
Nature, 605, 2022
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7W3M
 | | Structure of USP14-bound human 26S proteasome in substrate-inhibited state SD5_USP14 | | 分子名称: | 26S protease regulatory subunit 4, 26S protease regulatory subunit 6A, 26S protease regulatory subunit 6B, ... | | 著者 | Zhang, S, Zou, S, Yin, D, Wu, Z, Mao, Y. | | 登録日 | 2021-11-25 | | 公開日 | 2022-05-18 | | 最終更新日 | 2022-06-01 | | 実験手法 | ELECTRON MICROSCOPY (3.5 Å) | | 主引用文献 | USP14-regulated allostery of the human proteasome by time-resolved cryo-EM.
Nature, 605, 2022
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7W3I
 | | Structure of USP14-bound human 26S proteasome in substrate-inhibited state SB_USP14 | | 分子名称: | 26S protease regulatory subunit 4, 26S protease regulatory subunit 6A, 26S protease regulatory subunit 6B, ... | | 著者 | Zhang, S, Zou, S, Yin, D, Wu, Z, Mao, Y. | | 登録日 | 2021-11-25 | | 公開日 | 2022-05-18 | | 最終更新日 | 2022-06-01 | | 実験手法 | ELECTRON MICROSCOPY (3.5 Å) | | 主引用文献 | USP14-regulated allostery of the human proteasome by time-resolved cryo-EM.
Nature, 605, 2022
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6TUY
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2Y8O
 | | Crystal structure of human p38alpha complexed with a MAPK docking peptide | | 分子名称: | DUAL SPECIFICITY MITOGEN-ACTIVATED PROTEIN KINASE KINASE 6, MITOGEN-ACTIVATED PROTEIN KINASE 14 | | 著者 | Barkai, T, Garai, A, Toeroe, I, Remenyi, A. | | 登録日 | 2011-02-08 | | 公開日 | 2012-02-22 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | | 主引用文献 | Specificity of Linear Motifs that Bind to a Common Mitogen-Activated Protein Kinase Docking Groove.
Sci. Signal, 5, 2012
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6GU2
 | | CDK1/CyclinB/Cks2 in complex with Flavopiridol | | 分子名称: | 2-(2-chlorophenyl)-8-[(3~{R},4~{R})-1-methyl-3-oxidanyl-piperidin-4-yl]-5,7-bis(oxidanyl)chromen-4-one, Cyclin-dependent kinase 1, Cyclin-dependent kinases regulatory subunit 2, ... | | 著者 | Wood, D.J, Korolchuk, S, Tatum, N.J, Wang, L.Z, Endicott, J.A, Noble, M.E.M, Martin, M.P. | | 登録日 | 2018-06-19 | | 公開日 | 2018-12-05 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Differences in the Conformational Energy Landscape of CDK1 and CDK2 Suggest a Mechanism for Achieving Selective CDK Inhibition.
Cell Chem Biol, 26, 2019
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4ZZN
 | | Human ERK2 in complex with an inhibitor | | 分子名称: | 2-[[5-chloranyl-2-(oxan-4-ylamino)pyridin-4-yl]amino]-N-methyl-benzamide, MITOGEN-ACTIVATED PROTEIN KINASE 1, SULFATE ION | | 著者 | Ward, R.A, Colclough, N, Challinor, M, Debreczeni, J.E, Eckersley, K, Fairley, G, Feron, L, Flemington, V, Graham, M.A, Greenwood, R, Hopcroft, P, Howard, T.D, James, M, Jones, C.D, Jones, C.R, Renshaw, J, Roberts, K, Snow, L, Tonge, M, Yeung, K. | | 登録日 | 2015-04-10 | | 公開日 | 2015-05-27 | | 最終更新日 | 2015-08-26 | | 実験手法 | X-RAY DIFFRACTION (1.33 Å) | | 主引用文献 | Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of Erk1/2.
J.Med.Chem., 58, 2015
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2ZAZ
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4ZZM
 | | Human ERK2 in complex with an irreversible inhibitor | | 分子名称: | 7-ethylsulfonyl-N-(oxan-4-yl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-2-amine, MITOGEN-ACTIVATED PROTEIN KINASE 1, SULFATE ION | | 著者 | Ward, R.A, Colclough, N, Challinor, M, Debreczeni, J.E, Eckersley, K, Fairley, G, Feron, L, Flemington, V, Graham, M.A, Greenwood, R, Hopcroft, P, Howard, T.D, James, M, Jones, C.D, Jones, C.R, Renshaw, J, Roberts, K, Snow, L, Tonge, M, Yeung, K. | | 登録日 | 2015-04-10 | | 公開日 | 2015-05-27 | | 最終更新日 | 2015-08-26 | | 実験手法 | X-RAY DIFFRACTION (1.89 Å) | | 主引用文献 | Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of Erk1/2.
J.Med.Chem., 58, 2015
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