title: Development of a fluorescence intensity assay for the mitotic serine/threonine protein kinase Aurora-A.
abstract: 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.
authors.affiliation: Population Genetics, Cambridge, UK.
authors.forename: Andrew F
authors.initials: AF
authors.lastname: Slatter
authors.forename: Spencer
authors.initials: S
authors.lastname: Campbell
authors.forename: Richard M
authors.initials: RM
authors.lastname: Angell
mesh_terms: D064107:Aurora Kinase B; D064127:Aurora Kinases; D001667:Binding, Competitive / Q000187:drug effects; D002460:Cell Line; D004353:Drug Evaluation, Preclinical; D057166:High-Throughput Screening Assays; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D011485:Protein Binding / Q000187:drug effects; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D013050:Spectrometry, Fluorescence / Q000379:methods*
chemical_list: D008024:Ligands; D047428:Protein Kinase Inhibitors; C576921:AURKB protein, human; D064107:Aurora Kinase B; D064127:Aurora Kinases; D017346:Protein Serine-Threonine Kinases