The Aurora kinases are a group of serine/threonine protein kinases that regulate key steps during mitosis, and deregulation of these proteins (e.g., by gene amplification or overexpression) has been linked to a wide variety of tumor types. Thus, Aurora-A and Aurora-B have been intensely studied as targets for anticancer therapy and are now clinically validated targets. Here we report on the development of a novel fluorescence intensity binding assay for Aurora-A kinase inhibitors using a fluorescently labeled probe compound that shows intramolecular quenching when unbound but exhibits a dramatic increase in fluorescence when bound to Aurora-A.
Development of a Fluorescence Intensity Assay for the Mitotic Serine/Threonine Protein Kinase Aurora-A
Andrew F. Slatter,S. Campbell,R. Angell
Published 2013 in Journal of biomolecular screening
ABSTRACT
PUBLICATION RECORD
- Publication year
2013
- Venue
Journal of biomolecular screening
- Publication date
2013-02-01
- Fields of study
Biology, Medicine, Chemistry
- Identifiers
- External record
- Source metadata
Semantic Scholar, PubMed
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