1Z9X
 
 | | Human DRP-1 kinase, W305S S308A D40 mutant, crystal form with 3 monomers in the asymmetric unit | | Descriptor: | Death-associated protein kinase 2 | | Authors: | Kursula, P, Lehmann, F, Shani, G, Kimchi, A, Wilmanns, M. | | Deposit date: | 2005-04-05 | | Release date: | 2006-10-24 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (3.93 Å) | | Cite: | A structural insight into the double-locking mechanism of the human death-associated DRP-1 kinase
To be Published
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1ZOE
 | | Crystal structure of protein kinase CK2 in complex with TBB-derivatives inhibitors | | Descriptor: | 4,5,6,7-TETRABROMO-N,N-DIMETHYL-1H-BENZIMIDAZOL-2-AMINE, CHLORIDE ION, DIMETHYL SULFOXIDE, ... | | Authors: | Battistutta, R, Mazzorana, M, Sarno, S, Kazimierczuk, Z, Zanotti, G, Pinna, L.A. | | Deposit date: | 2005-05-13 | | Release date: | 2005-11-29 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.77 Å) | | Cite: | Inspecting the structure-activity relationship of protein kinase CK2 inhibitors derived from tetrabromo-benzimidazole.
Chem.Biol., 12, 2005
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1ZZL
 | | Crystal structure of P38 with triazolopyridine | | Descriptor: | 6-[4-(4-FLUOROPHENYL)-1,3-OXAZOL-5-YL]-3-ISOPROPYL[1,2,4]TRIAZOLO[4,3-A]PYRIDINE, Mitogen-activated protein kinase 14 | | Authors: | McClure, K.F, Han, S. | | Deposit date: | 2005-06-14 | | Release date: | 2005-09-13 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Theoretical and Experimental Design of Atypical Kinase Inhibitors: Application to p38 MAP Kinase.
J.Med.Chem., 48, 2005
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1ZYJ
 | | Human P38 MAP Kinase in Complex with Inhibitor 1a | | Descriptor: | 4-PHENOXY-N-(PYRIDIN-2-YLMETHYL)BENZAMIDE, Mitogen-activated protein kinase 14, octyl beta-D-glucopyranoside | | Authors: | Karpusas, M, Michelotti, E.L, Springman, E.B. | | Deposit date: | 2005-06-10 | | Release date: | 2005-11-08 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Two classes of p38alpha MAP kinase inhibitors having a common diphenylether core but exhibiting divergent binding modes.
Bioorg.Med.Chem.Lett., 15, 2005
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1ZZ2
 | | Two Classes of p38alpha MAP Kinase Inhibitors Having a Common Diphenylether Core but Exhibiting Divergent Binding Modes | | Descriptor: | Mitogen-activated protein kinase 14, N-[3-(4-FLUOROPHENOXY)PHENYL]-4-[(2-HYDROXYBENZYL)AMINO]PIPERIDINE-1-SULFONAMIDE, octyl beta-D-glucopyranoside | | Authors: | Michelotti, E.L, Moffett, K.K, Springman, E.B, Karpusas, M. | | Deposit date: | 2005-06-13 | | Release date: | 2005-10-18 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Two classes of p38alpha MAP kinase inhibitors having a common diphenylether core but exhibiting divergent binding modes.
Bioorg.Med.Chem.Lett., 15, 2005
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1XQZ
 | | Crystal Structure of hPim-1 kinase at 2.1 A resolution | | Descriptor: | Proto-oncogene serine/threonine-protein kinase Pim-1 | | Authors: | Qian, K.C, Wang, L, Hickey, E.R, Studts, J, Barringer, K, Peng, C, Kronkaitis, A, Li, J, White, A, Mische, S, Farmer, B. | | Deposit date: | 2004-10-13 | | Release date: | 2004-11-09 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Structural Basis of Constitutive Activity and a Unique Nucleotide Binding Mode of Human Pim-1 Kinase.
J.Biol.Chem., 280, 2005
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1XWS
 | | Crystal Structure of the human PIM1 kinase domain | | Descriptor: | 3-{1-[3-(DIMETHYLAMINO)PROPYL]-1H-INDOL-3-YL}-4-(1H-INDOL-3-YL)-1H-PYRROLE-2,5-DIONE, Proto-oncogene serine/threonine-protein kinase Pim-1, SULFATE ION | | Authors: | Knapp, S, Debreczeni, J, Bullock, A, von Delft, F, Sundstrom, M, Arrowsmith, C, Edwards, A, Guo, K. | | Deposit date: | 2004-11-02 | | Release date: | 2004-11-16 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Crystal structure of human PIM1 kinase domain
To be Published
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1ZYC
 | | Crystal Structure of eIF2alpha Protein Kinase GCN2: Wild-Type in Apo Form. | | Descriptor: | Serine/threonine-protein kinase GCN2 | | Authors: | Padyana, A.K, Qiu, H, Roll-Mecak, A, Hinnebusch, A.G, Burley, S.K. | | Deposit date: | 2005-06-09 | | Release date: | 2005-06-21 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Structural Basis for Autoinhibition and Mutational Activation of Eukaryotic Initiation Factor 2{alpha} Protein Kinase GCN2
J.Biol.Chem., 280, 2005
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1ZY4
 | | Crystal Structure of eIF2alpha Protein Kinase GCN2: R794G Hyperactivating Mutant in Apo Form. | | Descriptor: | GLYCEROL, Serine/threonine-protein kinase GCN2 | | Authors: | Padyana, A.K, Qiu, H, Roll-Mecak, A, Hinnebusch, A.G, Burley, S.K. | | Deposit date: | 2005-06-09 | | Release date: | 2005-06-21 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Structural Basis for Autoinhibition and Mutational Activation of Eukaryotic Initiation Factor 2{alpha} Protein Kinase GCN2
J.Biol.Chem., 280, 2005
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1ZWS
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1YDT
 | | STRUCTURE OF CAMP-DEPENDENT PROTEIN KINASE, ALPHA-CATALYTIC SUBUNIT IN COMPLEX WITH H89 PROTEIN KINASE INHIBITOR N-[2-(4-BROMOCINNAMYLAMINO)ETHYL]-5-ISOQUINOLINE | | Descriptor: | C-AMP-DEPENDENT PROTEIN KINASE, N-[2-(4-BROMOCINNAMYLAMINO)ETHYL]-5-ISOQUINOLINE SULFONAMIDE, PROTEIN KINASE INHIBITOR PEPTIDE | | Authors: | Engh, R.A, Girod, A, Kinzel, V, Huber, R, Bossemeyer, D. | | Deposit date: | 1996-07-24 | | Release date: | 1997-04-01 | | Last modified: | 2024-06-05 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity.
J.Biol.Chem., 271, 1996
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1YDS
 | | Structure of CAMP-dependent protein kinase, alpha-catalytic subunit in complex with H8 protein kinase inhibitor [N-(2-methylamino)ethyl]-5-isoquinolinesulfonamide | | Descriptor: | C-AMP-DEPENDENT PROTEIN KINASE, N-[2-(METHYLAMINO)ETHYL]-5-ISOQUINOLINESULFONAMIDE, PROTEIN KINASE INHIBITOR PEPTIDE | | Authors: | Engh, R.A, Girod, A, Kinzel, V, Huber, R, Bossemeyer, D. | | Deposit date: | 1996-07-24 | | Release date: | 1997-04-01 | | Last modified: | 2024-10-09 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity.
J.Biol.Chem., 271, 1996
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1YDR
 | | STRUCTURE OF CAMP-DEPENDENT PROTEIN KINASE, ALPHA-CATALYTIC SUBUNIT IN COMPLEX WITH H7 PROTEIN KINASE INHIBITOR 1-(5-ISOQUINOLINESULFONYL)-2-METHYLPIPERAZINE | | Descriptor: | 1-(5-ISOQUINOLINESULFONYL)-2-METHYLPIPERAZINE, C-AMP-DEPENDENT PROTEIN KINASE, PROTEIN KINASE INHIBITOR PEPTIDE | | Authors: | Engh, R.A, Girod, A, Kinzel, V, Huber, R, Bossemeyer, D. | | Deposit date: | 1996-07-24 | | Release date: | 1997-04-01 | | Last modified: | 2024-06-05 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity.
J.Biol.Chem., 271, 1996
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1YW2
 | | Mutated Mus Musculus P38 Kinase (mP38) | | Descriptor: | 2-(ETHOXYMETHYL)-4-(4-FLUOROPHENYL)-3-[2-(2-HYDROXYPHENOXY)PYRIMIDIN-4-YL]ISOXAZOL-5(2H)-ONE, Mitogen-activated protein kinase 14 | | Authors: | Laughlin, S.K, Clark, M.P, Djung, J.F, Golebiowski, A, Brugel, T.A, Sabat, M, Bookland, R.G, Laufersweiler, M.J, Vanrens, J.C, Townes, J.A, De, B, Hsieh, L.C, Xu, S.C, Walter, R.L, Mekel, M.J, Janusz, M.J. | | Deposit date: | 2005-02-16 | | Release date: | 2005-05-10 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.01 Å) | | Cite: | The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-alpha) production.
Bioorg.Med.Chem.Lett., 15, 2005
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1YXT
 | | Crystal Structure of Kinase Pim1 in complex with AMPPNP | | Descriptor: | PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, Proto-oncogene serine/threonine-protein kinase Pim-1 | | Authors: | Kumar, A, Mandiyan, V, Suzuki, Y, Zhang, C, Rice, J, Tsai, J, Artis, D.R, Ibrahim, P, Bremer, R. | | Deposit date: | 2005-02-22 | | Release date: | 2005-04-26 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Crystal structures of proto-oncogene kinase Pim1: a target of aberrant somatic hypermutations in diffuse large cell lymphoma.
J.Mol.Biol., 348, 2005
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1ZY5
 | | Crystal Structure of eIF2alpha Protein Kinase GCN2: R794G Hyperactivating Mutant Complexed with AMPPNP. | | Descriptor: | MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, Serine/threonine-protein kinase GCN2 | | Authors: | Padyana, A.K, Qiu, H, Roll-Mecak, A, Hinnebusch, A.G, Burley, S.K. | | Deposit date: | 2005-06-09 | | Release date: | 2005-06-21 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Structural Basis for Autoinhibition and Mutational Activation of Eukaryotic Initiation Factor 2{alpha} Protein Kinase GCN2
J.Biol.Chem., 280, 2005
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1ZXE
 | | Crystal Structure of eIF2alpha Protein Kinase GCN2: D835N Inactivating Mutant in Apo Form | | Descriptor: | GLYCEROL, Serine/threonine-protein kinase | | Authors: | Padyana, A.K, Qiu, H, Roll-Mecak, A, Hinnebusch, A.G, Burley, S.K. | | Deposit date: | 2005-06-07 | | Release date: | 2005-06-21 | | Last modified: | 2021-10-20 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Structural Basis for Autoinhibition and Mutational Activation of Eukaryotic Initiation Factor 2{alpha} Protein Kinase GCN2
J.Biol.Chem., 280, 2005
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1ZYS
 | | Co-crystal structure of Checkpoint Kinase Chk1 with a pyrrolo-pyridine inhibitor | | Descriptor: | N-{5-[4-(4-METHYLPIPERAZIN-1-YL)PHENYL]-1H-PYRROLO[2,3-B]PYRIDIN-3-YL}NICOTINAMIDE, SULFATE ION, Serine/threonine-protein kinase Chk1, ... | | Authors: | Stavenger, R.A, Zhao, B, Zhou, B.-B.S, Brown, M.J, Lee, D, Holt, D.A. | | Deposit date: | 2005-06-10 | | Release date: | 2006-06-13 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Pyrrolo[2,3-b]pyridines Inhibit the Checkpoint Kinase Chk1
To be Published
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2A27
 | | Human DRP-1 kinase, W305S S308A D40 mutant, crystal form with 8 monomers in the asymmetric unit | | Descriptor: | 2,3-DIHYDROXY-1,4-DITHIOBUTANE, Death-associated protein kinase 2 | | Authors: | Kursula, P, Lehmann, F, Shani, G, Kimchi, A, Wilmanns, M. | | Deposit date: | 2005-06-22 | | Release date: | 2006-10-10 | | Last modified: | 2024-05-29 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Human DRP-1 kinase, W305S S308A D40 mutant, crystal form with 8 monomers in the asymmetric unit
To be Published
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2A0C
 | | Human CDK2 in complex with olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor | | Descriptor: | 2-{[(2-{[(1R)-1-(HYDROXYMETHYL)PROPYL]AMINO}-9-ISOPROPYL-9H-PURIN-6-YL)AMINO]METHYL}PHENOL, Cell division protein kinase 2 | | Authors: | Krystof, V, McNae, I.W, Walkinshaw, M.D, Fischer, P.M, Muller, P, Vojtesek, B, Orsag, M, Havlicek, L, Strnad, M. | | Deposit date: | 2005-06-16 | | Release date: | 2006-01-24 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Antiproliferative activity of olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor
Cell.Mol.Life Sci., 62, 2005
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1YI4
 | | Structure of Pim-1 bound to adenosine | | Descriptor: | ADENOSINE, Proto-oncogene serine/threonine-protein kinase Pim-1 | | Authors: | Jacobs, M.D, Black, J, Futer, O, Swenson, L, Hare, B, Fleming, M, Saxena, K. | | Deposit date: | 2005-01-11 | | Release date: | 2005-01-25 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Pim-1 ligand-bound structures reveal the mechanism of serine/threonine kinase inhibition by LY294002.
J.Biol.Chem., 280, 2005
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1YQJ
 | | Crystal Structure of p38 Alpha in Complex with a Selective Pyridazine Inhibitor | | Descriptor: | 6((S)-3-BENZYLPIPERAZIN-1-YL)-3-(NAPHTHALEN-2-YL)-4-(PYRIDIN-4-YL)PYRAZINE, Mitogen-activated protein kinase 14, SULFATE ION | | Authors: | Tamayo, N, Liao, H, Goldberg, M, Syed, R, Li, V, Powers, D, Tudor, Y, Yu, V, Wong, M.L, Henkle, B, Middelton, S, Harvey, T, Jang, G, Hungate, R, Dominguez, C. | | Deposit date: | 2005-02-01 | | Release date: | 2005-04-26 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Design and synthesis of potent pyridazine inhibitors of p38 MAP kinase.
Bioorg.Med.Chem.Lett., 15, 2005
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1YRP
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1ZYD
 | | Crystal Structure of eIF2alpha Protein Kinase GCN2: Wild-Type Complexed with ATP. | | Descriptor: | ADENOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION, Serine/threonine-protein kinase GCN2 | | Authors: | Padyana, A.K, Qiu, H, Roll-Mecak, A, Hinnebusch, A.G, Burley, S.K. | | Deposit date: | 2005-06-09 | | Release date: | 2005-06-21 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.75 Å) | | Cite: | Structural Basis for Autoinhibition and Mutational Activation of Eukaryotic Initiation Factor 2{alpha} Protein Kinase GCN2
J.Biol.Chem., 280, 2005
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2A4L
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