MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors
| Autor: | Todd B. Sells, Ryan Chau, Jeffrey A. Ecsedy, Rachel E. Gershman, Kara Hoar, Jessica Huck, David A. Janowick, Vivek J. Kadambi, Patrick J. LeRoy, Matthew Stirling, Stephen G. Stroud, Tricia J. Vos, Gabriel S. Weatherhead, Deborah R. Wysong, Mengkun Zhang, Suresh K. Balani, Joseph B. Bolen, Mark G. Manfredi, Christopher F. Claiborne |
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| Rok vydání: | 2015 |
| Předmět: |
Kinase
business.industry INVESTIGATIONAL AGENTS Organic Chemistry Cell Aurora A kinase Pharmacology Biochemistry Clinical trial chemistry.chemical_compound medicine.anatomical_structure chemistry embryonic structures Drug Discovery Alisertib Medicine biological phenomena cell phenomena and immunity business Mitosis |
| Zdroj: | ACS Medicinal Chemistry Letters. 6:630-634 |
| ISSN: | 1948-5875 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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