3db8 | pdb_00003db8

Crystal structure of an activated (Thr->Asp) Polo-like kinase 1 (Plk1) catalytic domain in complex with Compound 041

spinqualitylabelsall models 3db8, resolution 3.15Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3db8 is a 1 chain structure with sequence from Brachidanio rerio. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: 1FR Related: 3d5w, 3db6, 3dbc, 3dbd, 3dbe, 3dbf Gene: plk1 (Brachidanio rerio) Activity: Polo kinase, with EC number 2.7.11.21 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMed A series of 2-amino-isoxazolopyridines was designed and synthesized as Polo-like kinase (Plk) inhibitors. Key SAR and crystallographic data are discussed. More advanced analogues inhibit Plk1 with good enzymatic activity and modest cell-based activity. Differential selectivity among the three Plk isoforms is observed. Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors.,Hanan EJ, Fucini RV, Romanowski MJ, Elling RA, Lew W, Purkey HE, VanderPorten EC, Yang W Bioorg Med Chem Lett. 2008 Oct 1;18(19):5186-9. Epub 2008 Aug 29. PMID:18790636 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Serine/threonine protein kinase

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