Aurora case study – six inhibitors and their action during cytokinesis
Aurora kinase inhibitors are a putative drug class for treating cancer. The Aurora kinase enzymes could be potential targets for novel small-molecule enzyme inhibitors.
Aurora kinases regulate cell cycle transit from G2 through cytokinesis, and thus are targets in cancer therapy.[1] There are three mammalian aurora kinase genes, encoding aurora A, B and C. Intense investigation has focused on aurora A and B as they appear to play a role in oncogenesis[2] with aurora A identified as a low penetrance tumor susceptibility gene in mice and humans.[3]
^Andrews, Paul D.; Knatko, Elena; Moore, William J.; Swedlow, Jason R. (2003). "Mitotic mechanics: The auroras come into view". Current Opinion in Cell Biology. 15 (6): 672–683. doi:10.1016/j.ceb.2003.10.013. PMID 14644191.
^Katayama, Hiroshi; Brinkley, W. R.; Sen, S. (2003). "The Aurora kinases: Role in cell transformation and tumorigenesis". Cancer and Metastasis Reviews. 22 (4): 451–464. doi:10.1023/a:1023789416385. PMID 12884918. S2CID 25350728.
^Ewart-Toland, Amanda; Briassouli, Paraskevi; De Koning, John P.; Mao, Jian-Hua; Yuan, Jinwei; Chan, Florence; Maccarthy-Morrogh, Lucy; Ponder, Bruce A J.; Nagase, Hiroki; Burn, John; Ball, Sarah; Almeida, Maria; Linardopoulos, Spiros; Balmain, Allan (2003). "Identification of Stk6/STK15 as a candidate low-penetrance tumor-susceptibility gene in mouse and human". Nature Genetics. 34 (4): 403–412. doi:10.1038/ng1220. PMID 12881723. S2CID 29442841.
Aurora kinase inhibitors are a putative drug class for treating cancer. The Aurora kinase enzymes could be potential targets for novel small-molecule enzyme...
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program is evaluating fadraciclib, a CDK2/9 inhibitor, and the anti-mitotic program CYC140, a PLK1 inhibitor, in patients with both solid tumors and hematological...
aneuploidy and also resistance to TAXOL . Excitingly, a small molecule inhibitor of Aurora A has shown antitumor effects in an in vivo model suggesting that...
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