4WHL
 
 | | A New Class of Peptidomimetics Targeting the Polo-box Domain of Polo-like kinase 1 | | Descriptor: | C6H5(CH2)8-DERIVATIZED PEPTIDE INHIBITOR, Serine/threonine-protein kinase PLK1 | | Authors: | Bang, J.K, Han, Y.H, Ahn, M.J, Lee, K.S. | | Deposit date: | 2014-09-23 | | Release date: | 2014-12-03 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2.71 Å) | | Cite: | A new class of peptidomimetics targeting the polo-box domain of polo-like kinase 1.
J.Med.Chem., 58, 2015
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4WHH
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3HIH
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3HIK
 | | Structure of human Plk1-PBD in complex with PLHSpT | | Descriptor: | 1,2-ETHANEDIOL, GLYCEROL, Pentamer phosphopeptide, ... | | Authors: | Wlodawer, A, Moulaei, T. | | Deposit date: | 2009-05-20 | | Release date: | 2009-06-09 | | Last modified: | 2017-11-01 | | Method: | X-RAY DIFFRACTION (1.77 Å) | | Cite: | Structural and functional analyses of minimal phosphopeptides targeting the polo-box domain of polo-like kinase 1.
Nat.Struct.Mol.Biol., 16, 2009
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3RQ7
 | | Polo-like kinase 1 Polo box domain in complex with a C6H5(CH2)8-derivatized peptide inhibitor | | Descriptor: | C6H5(CH2)8-derivatized peptide inhibitor, Serine/threonine-protein kinase PLK1 | | Authors: | Liu, F, Park, J.-E, Qian, W.-J, Lim, D.C, Graber, M, Berg, T, Yaffe, M.B, Lee, K.S, Burke Jr, T.R. | | Deposit date: | 2011-04-27 | | Release date: | 2011-07-20 | | Last modified: | 2012-12-12 | | Method: | X-RAY DIFFRACTION (1.55 Å) | | Cite: | Serendipitous alkylation of a Plk1 ligand uncovers a new binding channel.
Nat.Chem.Biol., 7, 2011
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3THB
 | | Structure of PLK1 kinase domain in complex with a benzolactam-derived inhibitor | | Descriptor: | 9-chloro-2-({5-[3-(dimethylamino)propyl]-2-methylpyridin-3-yl}amino)-5,7-dihydro-6H-pyrimido[5,4-d][1]benzazepine-6-thi one, Serine/threonine-protein kinase PLK1, ZINC ION | | Authors: | Sintchak, M.D. | | Deposit date: | 2011-08-18 | | Release date: | 2011-11-23 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Discovery of a Potent and Orally Bioavailable Benzolactam-Derived Inhibitor of Polo-Like Kinase 1 (MLN0905).
J.Med.Chem., 55, 2012
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3KB7
 | | Crystal structure of Polo-like kinase 1 in complex with a pyrazoloquinazoline inhibitor | | Descriptor: | 8-{[2-methoxy-5-(4-methylpiperazin-1-yl)phenyl]amino}-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide, L(+)-TARTARIC ACID, Serine/threonine-protein kinase PLK1, ... | | Authors: | Bossi, R.T, Bertrand, J.A. | | Deposit date: | 2009-10-20 | | Release date: | 2010-05-19 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors
J.Med.Chem., 53, 2010
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4J53
 | | Crystal structure of PLK1 in complex with TAK-960 | | Descriptor: | 4-[(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)benzamide, ACETATE ION, Serine/threonine-protein kinase PLK1, ... | | Authors: | Hosfield, D.J, Skene, R.J. | | Deposit date: | 2013-02-07 | | Release date: | 2013-05-29 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Discovery of TAK-960: An orally available small molecule inhibitor of polo-like kinase 1 (PLK1).
Bioorg.Med.Chem.Lett., 23, 2013
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4O6W
 | | Peptide-Based Inhibitors of Plk1 Polo-box Domain | | Descriptor: | Peptide-Based inhibitor, Serine/threonine-protein kinase PLK1 | | Authors: | Qian, W.-J, Park, J.-E, Lim, D.C, Park, S.-Y, Lee, K.-W, Yaffe, M.B, Lee, K.S, Burke, T.R. | | Deposit date: | 2013-12-23 | | Release date: | 2014-12-03 | | Method: | X-RAY DIFFRACTION (1.448 Å) | | Cite: | Mono-anionic phosphopeptides produced by unexpected histidine alkylation exhibit high plk1 polo-box domain-binding affinities and enhanced antiproliferative effects in hela cells.
Biopolymers, 102, 2014
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4LKM
 | | Crystal structure of Plk1 Polo-box domain in complex with PL-74 | | Descriptor: | GLYCEROL, PL-74, SULFATE ION, ... | | Authors: | Lee, W.C, Song, J.H, Kim, H.Y. | | Deposit date: | 2013-07-08 | | Release date: | 2013-12-11 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Exploring the binding nature of pyrrolidine pocket-dependent interactions in the polo-box domain of polo-like kinase 1
Plos One, 8, 2013
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4LKL
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2OGQ
 | | Molecular and structural basis of Plk1 substrate recognition: Implications in centrosomal localization | | Descriptor: | Serine/threonine-protein kinase PLK1 | | Authors: | Garcia-Alvarez, B, de Carcer, G, Ibanez, S, Bragado-Nilsson, E, Montoya, G. | | Deposit date: | 2007-01-08 | | Release date: | 2007-02-13 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Molecular and structural basis of polo-like kinase 1 substrate recognition: Implications in centrosomal localization.
Proc.Natl.Acad.Sci.Usa, 104, 2007
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4DFW
 | | Oxime-based Post Solid-phase Peptide Diversification: Identification of High Affinity Polo-like Kinase 1 (Plk1) Polo-box Domain Binding Peptides | | Descriptor: | CHLORIDE ION, Peptide, Serine/threonine-protein kinase PLK1 | | Authors: | Liu, F, Park, J.-E, Qian, W.-J, Lim, D, Gr ber, M, Berg, T, Yaffe, M.B, Lee, K.S, Burke Jr, T.R. | | Deposit date: | 2012-01-24 | | Release date: | 2012-03-28 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (1.55 Å) | | Cite: | Oxime-based Post Solid-phase Peptide Diversification: Identification of High Affinity Polo-like Kinase 1 (Plk1) Polo-box Domain Binding Peptides
Chem.Biol., 2012
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4O56
 | | Structure of PLK1 in complex with peptide | | Descriptor: | PHOSPHATE ION, Serine/threonine-protein kinase PLK1, synthetic peptide | | Authors: | Wang, T. | | Deposit date: | 2013-12-19 | | Release date: | 2014-12-24 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Integration of Charge-dipole Interaction and Intramolecular Hydrogen Bond in Ligand Design for the Polo-Box Domain of Polo-like Kinase 1
To be Published
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4O9W
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2OU7
 | | Structure of the Catalytic Domain of Human Polo-like Kinase 1 | | Descriptor: | ACETATE ION, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | Authors: | Ding, Y.-H, Kothe, M, Kohls, D, Low, S. | | Deposit date: | 2007-02-09 | | Release date: | 2007-04-24 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Structure of the catalytic domain of human polo-like kinase 1.
Biochemistry, 46, 2007
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2OWB
 | | Structure of the Catalytic Domain of Human Polo-like Kinase 1 | | Descriptor: | 4-(4-METHYLPIPERAZIN-1-YL)-N-[5-(2-THIENYLACETYL)-1,5-DIHYDROPYRROLO[3,4-C]PYRAZOL-3-YL]BENZAMIDE, ACETATE ION, Serine/threonine-protein kinase PLK1, ... | | Authors: | Ding, Y.-H, Kothe, M, Kohls, D, Low, S. | | Deposit date: | 2007-02-15 | | Release date: | 2007-04-24 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Structure of the catalytic domain of human polo-like kinase 1.
Biochemistry, 46, 2007
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4E9D
 | | The structure of the polo-box domain (PBD) of polo-like kinase 1 (Plk1) in complex with 3-(1-benzothiophen-2-yl)propanoyl-derivatized DPPLHSpTA peptide | | Descriptor: | 3-(1-benzothiophen-2-yl)propanoyl-derivatized DPPLHSpTA peptide, GLYCEROL, Serine/threonine-protein kinase PLK1 | | Authors: | Sledz, P, Hyvonen, M, Lang, S, Stubbs, C.J, Abell, C. | | Deposit date: | 2012-03-21 | | Release date: | 2012-10-10 | | Last modified: | 2012-12-12 | | Method: | X-RAY DIFFRACTION (2.75 Å) | | Cite: | High-throughput interrogation of ligand binding mode using a fluorescence-based assay.
Angew.Chem.Int.Ed.Engl., 51, 2012
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4J52
 | | Crystal structure of PLK1 in complex with a pyrimidodiazepinone inhibitor | | Descriptor: | 4-{[(7R)-9-cyclopentyl-7-ethenyl-7-fluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl]amino}-3-methoxy-N-(4-methylpiperazin-1-yl)benzamide, ACETATE ION, Serine/threonine-protein kinase PLK1, ... | | Authors: | Hosfield, D.J, Skene, R.J. | | Deposit date: | 2013-02-07 | | Release date: | 2013-05-29 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Discovery of TAK-960: An orally available small molecule inhibitor of polo-like kinase 1 (PLK1).
Bioorg.Med.Chem.Lett., 23, 2013
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4E67
 | | The structure of the polo-box domain (PBD) of polo-like kinase 1 (Plk1) in complex with hydrocinnamoyl-derivatized PLHSpTA peptide | | Descriptor: | Serine/threonine-protein kinase PLK1, hydrocinnamoyl-derivatized PLHSpTA peptide | | Authors: | Sledz, P, Hyvonen, M, Tan, Y.S, Lang, S, Spring, D, Abell, C, Best, R.B. | | Deposit date: | 2012-03-15 | | Release date: | 2012-10-10 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Using ligand-mapping simulations to design a ligand selectively targeting a cryptic surface pocket of polo-like kinase 1.
Angew.Chem.Int.Ed.Engl., 51, 2012
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4E9C
 | | The structure of the polo-box domain (PBD) of polo-like kinase 1 (Plk1) in complex with LDPPLHSpTA phosphopeptide | | Descriptor: | 2-(2-METHOXYETHOXY)ETHANOL, GLYCEROL, LDPPLHSpTA phosphopeptide, ... | | Authors: | Sledz, P, Hyvonen, M, Lang, S, Stubbs, C.J, Abell, C. | | Deposit date: | 2012-03-21 | | Release date: | 2012-10-10 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | High-throughput interrogation of ligand binding mode using a fluorescence-based assay.
Angew. Chem. Int. Ed. Engl., 51, 2012
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4RCP
 | | Crystal structure of Plk1 Polo-box domain in complex with PL-2 | | Descriptor: | 1,2-ETHANEDIOL, PL-2, Serine/threonine-protein kinase PLK1 | | Authors: | Lee, W.C, Song, J.H, Kim, H.Y. | | Deposit date: | 2014-09-16 | | Release date: | 2014-11-12 | | Last modified: | 2015-01-21 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | A new class of peptidomimetics targeting the polo-box domain of polo-like kinase 1.
J.Med.Chem., 58, 2015
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4HCO
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4HAB
 | | Crystal structure of Plk1 Polo-box domain in complex with PL-49 | | Descriptor: | 3-CYCLOHEXYL-1-PROPYLSULFONIC ACID, PHOSPHATE ION, PL-49, ... | | Authors: | Lee, W.C, Song, J.H, Kim, H.Y. | | Deposit date: | 2012-09-26 | | Release date: | 2013-04-03 | | Last modified: | 2022-12-21 | | Method: | X-RAY DIFFRACTION (2.65 Å) | | Cite: | Development of cyclic peptomer inhibitors targeting the polo-box domain of polo-like kinase 1.
Bioorg.Med.Chem., 21, 2013
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4H5X
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