| Structural highlights
2xru is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
| | Ligands: | |
| Related: | 1muo, 2x6d, 2j50, 2w1d, 1ol6, 2xne, 2bmc, 2c6e, 2j4z, 1ol5, 2x81, 2xng, 2c6d, 2wtw, 2wqe, 2w1c, 2w1g, 2wtv, 1ol7, 2w1e, 2w1f, 2x6e, 1mq4 |
| Activity: | Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 |
| Resources: | FirstGlance, OCA, 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 novel series of 3-amino-1H-thieno[3,2-c]pyrazole derivatives demonstrating high potency in inhibiting Aurora kinases was developed. Here we describe the synthesis and a preliminary structure-activity relationship, which led to the discovery of a representative compound (38), which showed low nanomolar inhibitory activity in the anti-proliferation assay and was able to block the cell cycle in HCT-116 cell line. This compound demonstrated favorable pharmacokinetic properties and good efficacy in the HL-60 xenograft tumor model.
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.,Bindi S, Fancelli D, Alli C, Berta D, Bertrand JA, Cameron AD, Cappella P, Carpinelli P, Cervi G, Croci V, D'Anello M, Forte B, Giorgini ML, Marsiglio A, Moll J, Pesenti E, Pittala V, Pulici M, Riccardi-Sirtori F, Roletto F, Soncini C, Storici P, Varasi M, Volpi D, Zugnoni P, Vianello P Bioorg Med Chem. 2010 Oct 1;18(19):7113-20. Epub 2010 Jul 25. PMID:20817473[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Bindi S, Fancelli D, Alli C, Berta D, Bertrand JA, Cameron AD, Cappella P, Carpinelli P, Cervi G, Croci V, D'Anello M, Forte B, Giorgini ML, Marsiglio A, Moll J, Pesenti E, Pittala V, Pulici M, Riccardi-Sirtori F, Roletto F, Soncini C, Storici P, Varasi M, Volpi D, Zugnoni P, Vianello P. Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity. Bioorg Med Chem. 2010 Oct 1;18(19):7113-20. Epub 2010 Jul 25. PMID:20817473 doi:10.1016/j.bmc.2010.07.048
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