Related Experiment Video

Updated: Apr 8, 2026

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
06:29

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells

Published on: July 30, 2020

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

Todd B Sells1, Ryan Chau1, Jeffrey A Ecsedy1

  • 1Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.

ACS Medicinal Chemistry Letters
|June 24, 2015
PubMed

Insights

Aurora kinases are vital for cell division, and their malfunction is linked to cancer. Investigational drugs MLN8054 and alisertib target Aurora A, with alisertib progressing through clinical trials for various cancers.

Area of Science:

  • Molecular Biology
  • Oncology
  • Pharmacology

Background:

  • Aurora kinases (A and B) are crucial regulators of cell mitosis.
  • Dysregulation of Aurora A and B is implicated in the development of human cancers.
  • Targeting Aurora kinases represents a promising strategy for cancer therapy.

Purpose of the Study:

  • To highlight the role of Aurora kinases in cell division and cancer.
  • To introduce investigational Aurora A inhibitors, MLN8054 and alisertib.
  • To discuss the clinical advancement of alisertib in cancer treatment.

Main Methods:

  • Identification and characterization of high-affinity, selective Aurora A inhibitors.
  • Preclinical evaluation of MLN8054 and alisertib.
  • Clinical trial assessment of alisertib in cancer patients.

Main Results:

  • MLN8054 and alisertib demonstrated high affinity and selectivity for Aurora A.
  • Both agents are orally bioavailable.
  • Alisertib has advanced into Phase II and III clinical trials.

Conclusions:

  • Aurora A inhibitors, such as alisertib, show therapeutic potential in oncology.
  • Alisertib's progression in clinical trials underscores its promise for treating hematological malignancies and solid tumors.
  • Targeting Aurora A is a viable strategy for novel cancer drug development.
Keywords:
AlisertibAurora A kinaseMLN8054MLN8237

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