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.
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| Ligands: | |
| 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, ProSAT |
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[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Hanan EJ, Fucini RV, Romanowski MJ, Elling RA, Lew W, Purkey HE, VanderPorten EC, Yang W. Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors. Bioorg Med Chem Lett. 2008 Oct 1;18(19):5186-9. Epub 2008 Aug 29. PMID:18790636 doi:10.1016/j.bmcl.2008.08.091
