Aurora Kinase Inhibitors for Cancer Research

Aurora kinases, a highly conserved class of enzymes, attach phospho-groups to Serine/Threonine residues of substrate proteins that take part in chromatid separation at the time of cell division. The human aurora kinase class includes three members: Aurora A, B, and C (AURKA, AURKB, and AURKC).

Kosigrim (talk) (Uploads)—Own work, Public Domain

Image credits: Kosigrim (talk) (Uploads)—Own work, Public Domain.

Functions of Human Aurora Kinase Family

Aurora A is essential for mitotic entry, centrosome functioning and duplication, and bipolar spindle assembly. Aurora B is the catalytic constituent of the chromosomal passenger complex, which directs events at the time of segregation of the chromatids during cytokinesis, mitosis, and histone modification (epigenetic regulation). Aurora C, which manifests in testes cells, is considered to be vital for chromosome segregation at the time of meiosis. The contribution of these kinases to cell division and deregulated manifestation of Aurora A and B in tumor cells (often leading to genetic abnormality and thereby resulting in malignancy) together offered the motivation to find and test small-molecule inhibitors of these kinases.

Most of these inhibitors are going through preclinical and clinical trials: MK-0457 (VX-680), AZD1152-HQPA, and PHA-739358. The first orally administered Aurora A kinase selective inhibitor was MLN8054, which was tested in human clinical trials for treating colorectal cancer. BioVision takes pride in delivering more than 25 aurora kinase inhibitors including the ones described in this article and more.

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BioVision develops and offers a wide variety of products including assay kits, antibodies, recombinant proteins & enzymes, and other innovative research tools for studying Apoptosis, Metabolism, Cell Proliferation, Cellular Stress, Cell Damage and Repair, Diabetes, Obesity and Metabolic Syndrome, Stem Cell Biology, Gene Regulation, Signal Transduction, etc. BioVision's products are currently being sold in more than 60 countries worldwide.

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Last updated: Feb 21, 2020 at 9:30 AM


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