Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays.

@article{Manfredi2011CharacterizationOA,
  title={Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays.},
  author={Mark G Manfredi and Jeffrey A. Ecsedy and Arijit Chakravarty and Lee Silverman and Mengkun Zhang and Kara M. Hoar and Stephen G. Stroud and Wei Hua Chen and Vaishali B. Shinde and Jessica J. Huck and Deborah R. Wysong and David A. Janowick and Marc L. Hyer and Patrick J Leroy and Rachel E. Gershman and Matthew D. Silva and Melissa Saylor Germanos and Joseph B. Bolen and Christopher F. Claiborne and Todd B. Sells},
  journal={Clinical cancer research : an official journal of the American Association for Cancer Research},
  year={2011},
  volume={17 24},
  pages={7614-24}
}
PURPOSE Small-molecule inhibitors of Aurora A (AAK) and B (ABK) kinases, which play important roles in mitosis, are currently being pursued in oncology clinical trials. We developed three novel assays to quantitatively measure biomarkers of AAK inhibition in vivo. Here, we describe preclinical characterization of alisertib (MLN8237), a selective AAK inhibitor, incorporating these novel pharmacodynamic assays. EXPERIMENTAL DESIGN We investigated the selectivity of alisertib for AAK and ABK and… CONTINUE READING
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