MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors
ACS Medicinal Chemistry Letters2015Vol. 6(6), pp. 630–634
Citations Over TimeTop 10% of 2015 papers
Todd B. Sells, Ryan Chau, Jeffrey Ecsedy, Rachel E. Gershman, Kara M. Hoar, Jessica J. Huck, David A. Janowick, Vivek J. Kadambi, Patrick Leroy, Matthew Stirling, Stephen G. Stroud, Tricia J. Vos, Gabriel S. Weatherhead, Deborah R. Wysong, Mengkun Zhang, Suresh K. Balani, Joseph B. Bolen, Mark Manfredi, Christopher F. Claiborne
Abstract
The Aurora kinases are essential for cell mitosis, and the dysregulation of Aurora A and B have been linked to the etiology of human cancers. Investigational agents MLN8054 (8) and alisertib (MLN8237, 10) have been identified as high affinity, selective, orally bioavailable inhibitors of Aurora A that have advanced into human clinical trials. Alisertib (10) is currently being evaluated in multiple Phase II and III clinical trials in hematological malignancies and solid tumors.
Related Papers
- → VX-680 Inhibits Aurora A and Aurora B Kinase Activity in Human Cells(2007)118 cited
- → Mitotic requirement for aurora A kinase is bypassed in the absence of aurora B kinase(2005)114 cited
- → Inhibition of Aurora A and Aurora B Is Required for the Sensitivity of HPV-Driven Cervical Cancers to Aurora Kinase Inhibitors(2017)24 cited
- MLN8054, an orally active Aurora A kinase small molecule inhibitor in phase I clinical trials(2006)
- → AT9283, a Small Molecule Multi-Targeted Kinase Inhibitor Induces Antimyeloma Activity Via Potent Aurora Kinase and STAT3 Inhibition.(2009)2 cited