Description
MLN8237 inhibits aurora kinase A (AurA) preventing mitotic spindle formation and proper completion of mitosis. MLN8237 exhibits anticancer chemotherapeutic activity and is currently in clinical trials as a potential treatment for multiple myeloma, non-Hodgkin’s lymphoma, and chronic lymphocytic leukemia (CLL). In bladder cancer cells, MLN8237 induces cell cycle arrest, aneuploidy, and apoptosis; in animal models of bladder cancer, this compound inhibits tumor growth. Additionally, MLN8237 inhibits tumor growth of neuroblastomas in vivo as well. In HUVECs, MLN8237 decreases tubule formation and inhibits VEGF secretion, suggesting potential anti-angiogenic activity.
References
Romain C, Paul P, Kim KW, et al. Targeting Aurora kinase-A downregulates cell proliferation and angiogenesis in neuroblastoma. J Pediatr Surg. 2014 Jan;49(1):159-65. PMID: 24439602.
Kelly KR, Shea TC, Goy A, et al. Phase I study of MLN8237-investigational Aurora A kinase inhibitor-in relapsed/refractory multiple myeloma, Non-Hodgkin lymphoma and chronic lymphocytic leukemia. Invest New Drugs. 2013 Dec 20. [Epub ahead of print]. PMID: 24352795.
Zhou N, Singh K, Mir MC, et al. The investigational Aurora kinase A inhibitor MLN8237 induces defects in cell viability and cell-cycle progression in malignant bladder cancer cells in vitro and in vivo. Clin Cancer Res. 2013 Apr 1;19(7):1717-28. PMID: 23403633.
