| Structural highlights
3dbe 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: | |
| Related: | 3d5w, 3db6, 3db8, 3dbc, 3dbd, 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-pyrazolopyridines was designed and synthesized as Polo-like kinase (Plk) inhibitors based on a low micromolar hit. The SAR was developed to provide compounds exhibiting low nanomolar inhibitory activity of Plk1; the phenotype of treated cells is consistent with Plk1 inhibition. A co-crystal structure of one of these compounds with zPlk1 confirms an ATP-competitive binding mode.
Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors.,Fucini RV, Hanan EJ, Romanowski MJ, Elling RA, Lew W, Barr KJ, Zhu J, Yoburn JC, Liu Y, Fahr BT, Fan J, Lu Y, Pham P, Choong IC, VanderPorten EC, Bui M, Purkey HE, Evanchik MJ, Yang W Bioorg Med Chem Lett. 2008 Oct 15;18(20):5648-52. Epub 2008 Aug 29. PMID:18793847[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Fucini RV, Hanan EJ, Romanowski MJ, Elling RA, Lew W, Barr KJ, Zhu J, Yoburn JC, Liu Y, Fahr BT, Fan J, Lu Y, Pham P, Choong IC, VanderPorten EC, Bui M, Purkey HE, Evanchik MJ, Yang W. Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5648-52. Epub 2008 Aug 29. PMID:18793847 doi:10.1016/j.bmcl.2008.08.095
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