Aurora Kinase Inhibitors
Aurora kinases are a highly conserved family of enzymes which add phospho-groups to Serine/Threonine residues of substrate proteins functioning in chromatid segregation during cell division. The human aurora kinase family comprises three members: Aurora A, B and C (AURKA, AURKB and AURKC). Aurora A is important in centrosome function and duplication, mitotic entry and bipolar spindle assembly. Aurora B is the catalytic component of the chromosomal passenger complex which coordinates events during segregation of the chromatids during mitosis, histone modification (epigenetic regulation) and cytokinesis. Aurora C is expressed in testes cells and is believed to be important for chromosome segregation during meiosis. The involvement of these kinases in cell division and deregulated expression of aurora A and B in tumor cells (often resulting in genetic aberrations and thus leading to malignancy) together provided the incentive to identify and test small-molecule inhibitors of these kinases. Many of these inhibitors are undergoing preclinical and clinical trials: MK-0457 (VX-680), AZD1152-HQPA, PHA-739358. MLN8054 was the first orally administered Aurora A kinase selective inhibitor to be tested in human clinical trials for the treatment of colorectal cancer. BioVision proudly offers several aurora kinase inhibitors including the ones mentioned above and more.
