Slatter Andrew F, Campbell Spencer, Angell Richard M
Population Genetics, Cambridge, UK.
J Biomol Screen. 2013 Feb;18(2):219-25. doi: 10.1177/1087057112459888. Epub 2012 Sep 14.
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.
极光激酶是一组丝氨酸/苏氨酸蛋白激酶，可调节有丝分裂过程中的关键步骤，这些蛋白质的失调（例如，通过基因扩增或过表达）与多种肿瘤类型有关。因此，极光激酶A和极光激酶B作为抗癌治疗靶点受到了深入研究，并且现在已成为临床验证的靶点。在此，我们报告了一种用于极光激酶A抑制剂的新型荧光强度结合测定法的开发，该方法使用一种荧光标记的探针化合物，该化合物在未结合时显示分子内淬灭，但在与极光激酶A结合时荧光会显著增加。
