MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors

[Image: see text] 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 inhibit...

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Autores principales: Sells, Todd B., Chau, Ryan, Ecsedy, Jeffrey A., Gershman, Rachel E., Hoar, Kara, Huck, Jessica, Janowick, David A., Kadambi, Vivek J., LeRoy, Patrick J., Stirling, Matthew, Stroud, Stephen G., Vos, Tricia J., Weatherhead, Gabriel S., Wysong, Deborah R., Zhang, Mengkun, Balani, Suresh K., Bolen, Joseph B., Manfredi, Mark G., Claiborne, Christopher F.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2015
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4468408/
https://www.ncbi.nlm.nih.gov/pubmed/26101564
http://dx.doi.org/10.1021/ml500409n
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author Sells, Todd B.
Chau, Ryan
Ecsedy, Jeffrey A.
Gershman, Rachel E.
Hoar, Kara
Huck, Jessica
Janowick, David A.
Kadambi, Vivek J.
LeRoy, Patrick J.
Stirling, Matthew
Stroud, Stephen G.
Vos, Tricia J.
Weatherhead, Gabriel S.
Wysong, Deborah R.
Zhang, Mengkun
Balani, Suresh K.
Bolen, Joseph B.
Manfredi, Mark G.
Claiborne, Christopher F.
author_facet Sells, Todd B.
Chau, Ryan
Ecsedy, Jeffrey A.
Gershman, Rachel E.
Hoar, Kara
Huck, Jessica
Janowick, David A.
Kadambi, Vivek J.
LeRoy, Patrick J.
Stirling, Matthew
Stroud, Stephen G.
Vos, Tricia J.
Weatherhead, Gabriel S.
Wysong, Deborah R.
Zhang, Mengkun
Balani, Suresh K.
Bolen, Joseph B.
Manfredi, Mark G.
Claiborne, Christopher F.
author_sort Sells, Todd B.
collection PubMed
description [Image: see text] 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.
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spelling pubmed-44684082016-06-11 MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors Sells, Todd B. Chau, Ryan Ecsedy, Jeffrey A. Gershman, Rachel E. Hoar, Kara Huck, Jessica Janowick, David A. Kadambi, Vivek J. LeRoy, Patrick J. Stirling, Matthew Stroud, Stephen G. Vos, Tricia J. Weatherhead, Gabriel S. Wysong, Deborah R. Zhang, Mengkun Balani, Suresh K. Bolen, Joseph B. Manfredi, Mark G. Claiborne, Christopher F. ACS Med Chem Lett [Image: see text] 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. American Chemical Society 2015-04-22 /pmc/articles/PMC4468408/ /pubmed/26101564 http://dx.doi.org/10.1021/ml500409n Text en Copyright © 2015 American Chemical Society This is an open access article published under an ACS AuthorChoice License (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) , which permits copying and redistribution of the article or any adaptations for non-commercial purposes.
spellingShingle Sells, Todd B.
Chau, Ryan
Ecsedy, Jeffrey A.
Gershman, Rachel E.
Hoar, Kara
Huck, Jessica
Janowick, David A.
Kadambi, Vivek J.
LeRoy, Patrick J.
Stirling, Matthew
Stroud, Stephen G.
Vos, Tricia J.
Weatherhead, Gabriel S.
Wysong, Deborah R.
Zhang, Mengkun
Balani, Suresh K.
Bolen, Joseph B.
Manfredi, Mark G.
Claiborne, Christopher F.
MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors
title MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors
title_full MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors
title_fullStr MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors
title_full_unstemmed MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors
title_short MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors
title_sort mln8054 and alisertib (mln8237): discovery of selective oral aurora a inhibitors
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4468408/
https://www.ncbi.nlm.nih.gov/pubmed/26101564
http://dx.doi.org/10.1021/ml500409n
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