| Ligand in Aurora B active site. Docking example from OTAVAchemicals/Life Chemicals Aurora B focused library. The detection of H-bonds between ligand and key Aurora B residue (Ala173) was used for the library preparation.
| The serine/theronine protein kinases of aurora family genes play a critical role in the regulation of key cell cycle processes. Aurora B mediates chromosome segregation by ensuring orientation of sister chromatids and overexpression of Aurora B in diploid human cells NHDF (normal human diploid fibroblast) induces multinuclearity. In human thyroid carcinomas, cell lines originating from different histotypes showed an increase in Aurora B expression. Immunohistochemical analysis of archive samples showed a high expression of Aurora B in anaplastic thyroid carcinomas; conversely, Aurora B expression was not detectable in normal thyroid tissue. Real-time PCR analysis confirmed a strong expression of Aurora B in anaplastic thyroid carcinomas. The block of Aurora B expression induced by RNA interference or by using an inhibitor of Aurora kinase activity significantly reduced the growth of thyroid anaplastic carcinoma cells. The focused libraries, including docking scores and drug-like properties, are available on request. Feel free to contact us! Sorrentino et al. Aurora B overexpression associates with the thyroid carcinoma undifferentiated phenotype and is required for thyroid carcinoma cell proliferation. J Clin Endocrinol Metab. 2005 Feb;90(2):928-35. Epub 2004 Nov 23.
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