Quantitative conformational profiling of kinase inhibitors reveals origins of selectivity for Aurora kinase activation states [Biochemistry]

Protein kinases undergo large-scale structural changes that tightly regulate function and control recognition by small-molecule inhibitors. Methods for quantifying the conformational effects of inhibitors and linking them to an understanding of selectivity patterns have long been elusive. We have developed an ultrafast time-resolved fluorescence methodology that tracks structural movements of...

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